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Effective Malaria Treatment Is Fraught With Challenges
Effective malaria treatment is fraught with challenges. Resistance is seemingly around the corner for every previously superlative drug, while being
deeply entrenched among those medications that a few decades ago were vital to chemotherapy. For artemisinin, the first signs of resistance were
observed in a 2008 study of parasite clearance times following monotherapy with artesunate. Clearance was slower among patients from the Eastern
Thai–Cambodian border than that of patients from the Thai–Myanmar border to the West (Dondorp et al., 2009). Though an alarming fact on its own,
when coupled with the proportional increase of such slow–clearing infections from 0.6% in 2001 to 20% in 2010 with rates approaching 42% in
Cambodia one must conclude that there is cause for alarm (Flannery et al., 2013). Resistance is not only emerging but also spreading. Now more than
ever we have need of new medicines as well as new approaches for producing those medicines. The link to plant physiology among Plasmodium spp. is
basically irrefutable and imperatively needs further investigating. By elucidating essential biosynthetic pathways behind such compounds like abscisic
acid, we can find hitherto unknown targets as well as broaden our knowledge of the evasion mechanisms that are at the disposal of our protozoan foes.
Evasion is the primary response of malaria in response to the immune system's efforts and this tactic appears to have been extended to one of the most
powerful drugs we have.
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Verapamil Research Paper
Verapamil has 4 different kind of dosage form which orally in tablet, tablet controlled release, capsule extended release and injection form. The
ingredient for making tablet has pharmacological action is verapamil hydrochloride. Each tablet oral contains 40mg, 80mg, 120mg and 160 mg of the
active ingredient. The other excipients are magnesium stearate, propylene glycol, sunset yellow aluminium lake, quinoline yellow aluminium lake,
titanium dioxide, microcrystalline cellulose, hydroxypropylcellulose and methylhydroxypropylcellulose. Beware using sunset yellow aluminum lake
because it can cause allergic reactions. The steady state has to be controlled to obtain optimal therapeutic effect and also patient compliance needs to be
considered. Therefore, controlled... Show more content on Helpwriting.net ...
Due to HPMC is a pH–independent polymer, it sustain the drug release by hydrating to form a gel layer at the surface of the tablet. Sodium alginate is a
pH–dependent, when exposed to acidic in stomach; it will convert to insoluble alginic acid. By the way, the type and amount of polymer affected the
release of drug. For both forms of tablets usually should be stored in tight, light–resistance container or amber glass at 15–25 oc. The shelf life is three
years from the date of manufacturing. For capsule extended release oral contains 100mg, 120mg, 180mg, 200mg, 240mg, 300mg and 360mg of the
active ingredient. These forms using the diffusion delivery system which are consists of controlled–release coated pellets enclosed in a hard gelatin
capsule. Polymers can be using both water soluble and water–insoluble polymers. When exposed to water in GI tract, the soluble polymer will slowly
dissolves, allow the drug to diffuse while the insoluble polymer act as barrier maintaining controlled release of the drug into GI tract. It should be
stored in tight light–closed container at room temperature
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Acts : Discussion : Artemisinin-Based Combination Therapies
Discussion Artemisinin–based combination therapies (ACTs) are currently considered gold standard in the management of uncomplicated malaria. For
the liver stages, primaquine is the only drug approved to eliminate hypnozoites. Resistance against existing antimalarials is well documented, and
troubling due to the emerging resistance to artemisinins. Therefore, a rising incidence of drug resistance requires the development new drugs, with
novel disease targeting strategies. Moreover, the challenge is to develop innovative drugs that demostrate (i) faster onset and longer duration of drug
action, (ii) safe for children and pregnant women, and (iii) ideally be amenable to a single–dose administration. Following are brief descriptions of such
... Show more content on Helpwriting.net ...
Ferroquine, unlike chloroquine, accumulates in the digestive vacuole of the chloroquine resistant parasites, enabling P. falciparum chloroquine
resistance transporter, PfCRT inhibition. [6] 3.Amodiaquine is also active against most chloroquine resistant strains, however, two reactive metabolites
are formed, namely imine and aldehyde, and are the likely cause of the hepatotoxicity and agranulocytosis, respectively. [7] 4.N–tert–Butyl isoquine
(GSK369796) was designed to avoid the formation of quinone imines, and has entered Phase I studies. It is potent in vitro, including in the chloroquine
resistant strain K1 (EC50 = 13 nM) and is active in vivo with an ED50 = 3.8 mg/kg/day, thus being comparable to amodiaquine. In spite of the excellent
exposures and near quantitative oral bioavailabilities in animal models, its development was discontinued due to exposures insufficient to demonstrate
drug safety superior to chloroquine. [8] 5.In an effort to select the next generation of quinoline methanol derivatives that could serve as a replacement
for mefloquine, the Walter Reed Army Institute of Research screened for analogs with a lower brain penetration, and identified WR621308, which has
a substantially lower permeability across MDCK cell monolayers than mefloquine, suggesting lower brain exposures. [9] 6.Cycloguanil and
pyrimethamine demonstrate inhibition of dihydrofolate reductase (DHFR).
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Target For Schizophrenia Essay
PDE10A–A target for schizophrenia? Phosphodiesterases (PDEs) are a class of enzymes, which are responsible for the breakdown of phosphodiester
bonds, specifically hydrolysing cyclic nucleotides, like the secondary messenger molecules cyclic adenosine monophosphate (cAMP) and cyclic
guanosine monophosphate (cGMP) in the striatal region of the brain.1 Via their control of both cAMP and cGMP in the cell, PDEs contribute to cell
signalling making them potentially important drug targets.2 This enzyme class consists of 11 different families, PDE1 to PDE11, which vary in
sequence homology, domain architecture and sequence homology.1 PDE10A is a PDE of current interest as a possible target to treat neurological
diseases such as Schizophrenia and... Show more content on Helpwriting.net ...
The active site contains residues that form complementary interactions to MP–10 (Figure 3B), there are several hydrophobic interactions, from certain
amino acid residues in the active site of PDE10A to the MP–10 inhibitor, in particularly the quinoline and pyridine moieties. There are also two
hydrogen bonds between the active site and MP–10, which is via the phenol group (donor) on the tyrosine (Tyr683) residue to the nitrogen (acceptor) in
the quinoline moiety and to the ether oxygen (acceptor) within MP–10.6 Chemoproteomics Demonstrates Target Engagement and Exquisite Selectivity
of the Clinical Phosphodiesterase 10A Inhibitor MP–10 in Its Native Environment The study, by SchuМ€lke et al. aimed to provide information that
enables further development of chemical biology probes for important classes of enzymes, particularly focussing on developing a chemical probe for
the PDE10A enzyme. To characterise the target engagement of MP–10, SchuМ€lke et al. designed a photoaffinity probe for PDE10A which contained
a linker attached to the PDE10A recognition element (Figure 4), so that a reporter group could be introduced without effecting the proteins activity.
The group decided, via studying the cocrystal structure, that the pyrazole nitrogen would be the best site for linker attachment as it is unsubstituted and
a relatively synthetically accessible point of modification. Adding to
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The Epidemic Of Vibrio Cholera
Vibrio cholera is a gram negative rod shaped bacteria which colonises the human gut causing acute diarrheal disease and leads to frequent epidemics
around the world. In 2014 190, 549 cholera cases were reported to the World Health Organisation (Global Health Observatory Data 2014) , however
the true number is likely to be far higher as there are many greatly affected locations which have poor or nonexistent data. Vibrio cholera is currently
treated by the use of oral antibiotics coupled with rehydration therapy however the bacteria are now developing resistance and new treatments must be
produced in order to prevent further epidemics and unnecessary deaths. This essay will discuss the pathogenesis of Vibrio cholera bacteria along with
antibiotic treatment of cholera and its methods of antibiotic resistance. There are twenty known groups of the vibrio cholera bacteria however, group
V.cholerae 01 and group V.cholerae 0139 only are capable of causing epidemics. The main causes for the spread of these strains to cause epidemics are
transmission via drinking untreated water from a water source with similar conditions to the where the organism would naturally grow, or via eating or
drinking produce contaminated by the faeces of infected people. Once ingested pathogenesis occurs. The bacteria enter the human gut and begin to
colonise the small intestine. Their flagella provide motility and digestive enzymes such as mucinase, a mucolytic enzyme which depolymerises mucus,
allow
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Hydrazino-Spengler Essay
8.Hydrazino–Pictet–Spengler ligation reaction = In this reaction, the aliphatic and aromatic hydrazines are used as a substrate to undergo
pictet–spengler reaction with aldehydic and ketonic group. As described in the above category 7, the various substrates are used for ligation with
aldehydic and ketonic groups of the proteins, P. Agarwal and research group developed the Hydrazino–Pictet–Spengler(HIPS) ligation reaction so that
the stable protein conjugates can be developed . This strategy can be used in the development of a prodrug delivery system. The advantage of this
scheme over the other oxime and hydrazone ligations is that the ligation proceeds very fast near the neutral pH(that is the pH of the normal
physiological body) and the product of the HIPS ligation is showing very long stability in human plasma (approx 5 days) as compared to that of
oxime–linked conjugate (approx 1 day). This was monitered by protein–fluorophore conjugates by ELISA(42). Scheme 18. Overview of the
Hydrazino–Pictet–Spengler reaction. A) In reaction with a small molecule and B) protein aldehydes, a Cв€’C bond (highlighted in red) is formed
between the indole and the aldehyde of interest ... Show more content on Helpwriting.net ...
It is a very important reaction for the synthesis of the larged fused heterocyclic compounds. Researchers have developed a lot of series of fused
heterocycles and analyzed them for their physiological and therapeutic effect. Many new drugs are there in the market that are being synthesised from
this valuable and novel reaction. The researchers have also undergone experiments regarding the effect of using various types of substrates, solvent
system, catalyts, temperature and many other parameters on the rate and yield of the reaction. Still a lot of research work is being going on to bring
the modifications in the reations. In short, this reaction has a bright future aspects in terms of research
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Organic Food Research Papers
Food directly affects to human health; it supplies energy for human activities. Now, choosing good foods for family becomes a hard problem with
many households when people hear about the toxic ingredients in food every day. The diseases, which have been linked to food poisoning, are
increasing day by day. The development of new technology analyzed the nutrient elements, and figured out the risks of poisonous elements in food. The
scientists researched a new farming method called organic farming method that is producing the best quality food for every person. Nowadays, organic
food has become a familiar term with many people. People should consume organic food because it reduces health risks, tastes great, protects the
environment, and ... Show more content on Helpwriting.net ...
For instance, the effect on cells is up to four times when Brilliant Blue and MSG are combined. It will go up to seven times when Quinoline Yellow and
Aspartame are combined together (Lee par. 6). The reason of diarrhea is from remaining toxic elements, which cannot be cleaned by rinsing. Moreover,
organic foods have more nutritional elements. Those are essential ingredients, which enhance people's health. According to the Organic Consumers
Association, organic food has 25% more nutrition in terms of vitamins and minerals than products derived from industrial agriculture. Organic products
have higher level of beta–carotene, vitamin A, D, E, essential acids, and essential minerals ("Why We" par. 1
–2). Furthermore, organic farming method
also protects the farmers and the pickers who are working and contacting with pesticides everyday on the farm. The consumers protect the farmers
indirectly, and protect themselves directly because organic food does not contain pesticides. In 2007, according to the United States Environmental
Protection Agency data, the amount of pesticide active ingredient used in farming in the U.S. is 1,133 million pounds (3). It is true that the remaining
pesticides can be removed after washing in some kind of fruit and veggies, but it is only a small proportion. The remaining pesticides in non–organic
food cannot be removed after washing especially in thinner skin fruit such as strawberries,
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Coal Tar Production Essays
Production
The complete process of coal tar production is shown in Figure 1. The coal tar is produced by carbonization of coal. In this process, the coal is heated
at 900–1100 ВєC and the evolved vapors are condensed to form liquid, from which ammonia is removed to obtain a black viscous crude coal tar. The
composition of tar so obtained depends upon the origin and composition of starting material used viz. bituminous (soft) coal, anthracite (hard) (Arnold
1997, Thami 2002).
Crude coal tar can be further purified using various techniques viz. solvent extraction, fractional distillation or coloum chromatography. The extraction
of crude coal tar with alcohol containing 5% w/w Tween 80 produces Liquor carbonis detergens (LCD). Similarly, the... Show more content on
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Characterization
It is most commonly analyzed with either Liquid Chromatography having Ultraviolet/ Fluorescence detection (HPLC/UV, HPLC/FD) or Gas
Chromatography coupled with Mass Spectroscopy (GS–MS) (EPA 1994; Litofsky1999; Gruber et. al., 1970). Both the techniques offer high sensitivity
and selectivity. However, the high cost of equipment and long run time, especially for LC, are the barriers for their utilization in routine analysis. The
other techniques which can be been explored to characterize the coal tar are Spectrofluorimetry (Li 1994, Raza 2012,), Nuclear magnetic resonance
(NMR) and Fourier Transform Infrared Spectroscopy (FTIR) (Nelson 1996, Cerny 1991).
Pharmacological action
Despite its long history of use and wide acceptance, the exact mechanism of action of coal tar is still elusive. Coal tar is known to posses keratolytic,
anti–pruitic, anti–mitotic, and anti inflamatory activities (Paghdal, 2009);; Roelofzen 2007). The researchers have put forward many theories to explain
these pharmacological actions viz. suppression of DNA synthesis, inhibition of sebum production, photosensitizing effects within the range of the
ultraviolet light A (UVA) and visible light spectrum (Gruper 1971, Arnold, 1997, Thami, 2002, Everett 1961, Kaidbey 1977). The constituents that are
thought to be responsible for these therapeutic dermatologic effects include the followings;
(1) Acridine compounds in the
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Kill Parasites Than Chloroquine As A Weekly Prophylaxis
2.2.2.2 Amodiaquine
Amodiaquine (Figure 2.3b) is another example of 4–aminoquinoline. It is similar with chloroquine, but it can more effectively kill parasites than
chloroquine, as well as a weekly prophylaxis. Because of the similar structure, amodiaquine is supposed to have the same antimalarial mechanism.
Hayeshi et al. [20.45] and Fley and Tilley[20.46] proved that amodiaquine can accumulate in digestive vacuole and bind to heme. Besides, an
incomplete cross–resistance has been found between amodiaquine and chloroquine, this may be due to the mutation of PfCRT and PfMDR1.
2.2.3 8–Aminoquinoline
2.2.3.1 Pamaquine
Pamaquine (Figure 2.5b) is an 8–aminoquinoline, synthesized based on the structure of methylene blue (Figure 2.5a). It is the first antimalarial drug
that has activity against liver stage parasites, and can prevent the relapse of P. vivaxmalaria. Although pamaquine can delay the first attachment of
malaria, it is an incomplete protection. So at that time, pamaquine was usually combined with quinine to treat malaria. However, pamaquine was
reported with severe toxicological concerns, relating with glucose 6–phosphate dehydrogenase (G6PD) deficiency, and it is not as efficient as
primaquine. Because of these problems, pamaquine is no longer used.
2.2.3.2 Primaquine
In 1940s, primaquine (figure 2.5c) was first synthesized by Elderfield[wiki.2]. Although it still has side effects for G6PD deficient patients just like
pamaquine, it can more efficiently treat P.
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Electrochemical And Quantum Chemical Studies Of The...
Electrochemical and quantum chemical studies of the corrosion and hydrogen evolution reaction of mild steel in acid medium
Rabab M. El–Sherif a,*, K. M. Zohdy b Sowmya Ramkumar c
a Cairo University, Faculty of Science, Department of chemistry, Giza, 12613, Egypt b Higher Technological Institute, 10th of Ramadan City, Egypt c
Department of chemistry, PSGR Krishnammal College for Women, Peelamedu, Coimbatore, India
Abstract
Electrochemical behavior and hydrogen evolution reaction of mild steel in sulfuric acid solutions, containing different concentrations of
gamma–Aminobutyric acid (GABA) as a green inhibitor have been investigated. The electrochemical techniques included Tafel polarization and
electrochemical impedance spectroscopy (EIS). The rate of both the corrosion reaction and the hydrogen evolution affected significantly by changing
GABA concentrations. Polarization results showed that GABA is a mixed type inhibitor with good inhibition efficiency. Increasing the temperature led
to an increase in the hydrogen evolution rate and a decrease in the total surface resistance value (RT) or the relative film thickness (1/CT) of the steel.
Quantum calculation including EHOMO, ELUMO, the energy gap (?E) and the fraction of transferred electrons (?N) demonstrated the inhibition
ability of GABA. The results were confirmed by surface examination using scanning electron microscopy. Adsorption of GABA on the steel surface
fitted the Langmuir isotherm. Thermodynamic parameters
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Artemisinin Based Combination Therapies ( Acts )
Artemisinin–based combination therapies (ACTs) are currently considered gold standards in the management of uncomplicated malaria. For the liver
stages, primaquine is the only drug approved to eliminate hypnozoites. Resistance against existing antimalarials is well documented, and troubling due
to the emerging resistance to artemisinins. Therefore, a rising incidence of drug resistance requires the development new drugs, with novel disease
targeting strategies. Moreover, the challenge is to develop innovative drugs that demostrate (i) faster onset and longer duration of drug action, (ii) safe
for children and pregnant women, and (iii) ideally be amenable to a single–dose administration. Following are brief descriptions of such innovative...
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2.Ferroquine was found to be active against chloroquine– resistant strains, and is currently undergoing Phase II clinical trials. Ferroquine, unlike
chloroquine, accumulates in the digestive vacuole of the chloroquine resistant parasites, enabling P. falciparum chloroquine resistance transporter,
PfCRT inhibition.
3.Amodiaquine is also active against most chloroquine resistant strains, however, two reactive metabolites are formed, namely imine and aldehyde, and
are the likely cause of the hepatotoxicity and agranulocytosis, respectively.
4.N–tert–Butyl isoquine (GSK369796) was designed to avoid the formation of quinone imines, and entered Phase I studies. It is potent in vitro,
including in the chloroquine resistant strain K1 (EC50 = 13 nM) and is active in vivo with an ED50 = 3.8 mg/kg/day, thus being comparable to
amodia– quine. In spite of the excellent exposures and near quantita– tive oral bioavailabili ties in animal models, its developmen t was discontinue d
due to exposures insufficient to demonstrate drug safety superior to chloroquine.
5.In an effort to select the next generation of quinoline methanol derivatives that could serve as a replacement for mefloquine, the Walter Reed Army
Institute of Research screened for analogs with a lower brain penetration, and identified WR621308, which has asubstantially lower permeability across
MDCK cell monolayers than mefloquine, suggesting lower brain
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MRSA: The Role Of Antibiotic Resistance In Bacteria
Lastly, but most importantly, antibiotic misuse needs to be avoided because it can lead to antibiotic resistance. Antibiotic resistance is a bacterium's
ability to overcome the effects of antibiotics and to survive in the presence of them ("About" par. 1). This is what causes antibiotics to be ineffective
towards some bacterial infections. When a bacteria is exposed to the same antibiotic regularly, that bacteria mutates to become antibiotic resistant.
Bacteria have many mechanisms of resistance. For instance, bacteria can achieve resistance by changing the chemical structure of their cell walls,
pumping the antibiotic out of their cell via pumps, and acquiring enzymes that inactivate antibiotics (Groopman 57). Since there are many ways ... Show
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While this may be true in some instances, it is a very dangerous approach to antibiotic use because of the many negative effects. As stated earlier, the
term "antibiotic" translates to "against life" because antibiotics are used to kill living organisms; therefore, if antibiotics are used irresponsibly and in
large quantities, they can kill humans. Further, the adverse effects caused by antibiotics may have negative consequences. For example, antibiotics
eliminate benign bacteria in the human colon, which allows opportunistic bacteria to take over (Sachs 191). As previously stated, this may cause many
complications such as Clostridium difficile infections, diarrhea, and fatal colon inflammation (Surawicz par.1,3). C. difficile is responsible for 29,000
deaths a year (Lessa, et. al. par. 18). That number is too great to overlook. Additionally, Antibiotics can cause Klebsiella, a bacteria that has a multidrug
resistant strain (Johnson 52). Furthermore, widespread antibiotic use will not cure every illness. Despite forty percent of people believing that
antibiotics can cure viral infections, antibiotics are only effective against bacterial infections ("Entrenched" par. 5). Lastly, widespread antibiotic use
leads to antibiotic resistance. Every year resistant bacteria are the cause of two million infections in the United States (Alic par. 2). If
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Ocular Melanoma Research Paper
While researching in depth Ocular Melanoma, there has been a consistent theme persisting there is not enough research done to find a way to decrease
metastasis percentage and increase survival rate. The current attempts at decreasing metastasis and increasing survival rate have stayed the same
throughout the course of 4 decades. The current drug, LS2616, is being used to treat Ocular Melanoma patients, but it is used to late to feel the full
impact of the drug. Research and Development laboratories are working on a faster–acting drug, but nothing has been tested on mice or released to the
public. If new drugs could be created, the survival rate of Ocular Melanoma would increase drastically.
History
Ocular Melanoma (OM) is a deadly killer. ... Show more content on Helpwriting.net ...
There are two main categories for treatment; radiation and surgery. The choice is ultimately up to the patient, but depending on the size and
location of the tumor, different treatments work better. Radiation and surgery treatments have both pros and cons. " Plaque radiation therapy is the
most common and effective radiation for ocular melanoma" ("Ocular Melanoma Treatment", 2016, para 4.). It can be distributed either by a
machine or by a gold plaque, that resembles a lot like a tiny bottle cap. Removing the tumor surgically or removing the eye all together are the two
most common surgical methods. If the tumor is small, then just the tumor can be removed, if it is in the correct location to remove it without
damaging any other part of the eye. "If the tumor is large... and cause severe eye pain" the whole eye will be removed, medically referred to as
enucleation ("Treating Uveal (Eye) Melanoma by Location and Size", 2017, para. 8). Once the removal of the eye occurs, after the patient heals, they
would be fitted for a prosthetic eye that matches your other eye. The artificial eye can move, and resemble a real eye, but the patient will just lose their
vision. Both radiation and surgery can result in sickness, much symptoms like the flu, and can sometimes lead to the loss of total vision. If the tumor
metastasizes to the liver, there are treatments to try and reduce more metastasis and decrease the tumor, as well as after/before enucleation to try and
stop metastasis. If the tumor is present, but has not metastasized, the oncologist can prescribe medication to prevent metastasis. "LS 2616, a quinoline
3–carboxamide... decrease in primary and secondary tumor's growth and metastasis" (Harning, 1988, p.1). It can slow the growth of the tumor that
metastasized to the liver, the goal overall is to stop more metastases from
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Pharmacological And Ethnobotanical Review Of Aristolochia...
Pharmacological and Ethnobotanical review of Aristolochia bracteolata L. (Aristolochiaceae)
M. B. Patil Department of Botany, J.E.S's, Arts, Science and Commerce College, Nandurbar
E–mail; drmadhukarpatil@gmail.com
Abstract The present study deals with review of pharmacological and ethnobotanical uses of Aristolochia bracteolata L. from family Aristolochiaceae is
commonly known as Kida–mari, Gidan–pala. The plant has been used widely by traditional practitioners for the treatment of various diseases in in
Indian subcontinent in the traditional system of medicine to treat cholera, fever, bowel troubles, ulcers, leprosy, skin diseases, menstrual problems and
snakebites. The plant is also used as emmenagogue, abortifacient, antineoplastic, antiseptic, anti–inflammatory, antimicrobial, antipyretic, antifertility
and antispermatogenic agent. Aristolochic acid, a major active constituent of the plant is reported to cause cancer, nephropathy, sister chromatid
exchange and is a potent abortifacient. Aristolochia species are also used in China, Philippines, Cuba, Nigeria, East and West Africa, Caribbean island,
and sub tropical countries as a folk medicine to treat eczema, rheumatic pain, stomachic, earache, syphilis and gonorrhea. The plants also used in the
treatment of domestic animals. The present review deals with the different scientific studies and reports available in different aspects of this plant in the
areas of Morphology, Phytochemistry, Pharmacology,
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Trimethoxynicotinonitrile Essay
11– 4,5,6–Trimethoxynicotinonitrile–2–thion (39) was prepared through the multicomponent, condensation of acetaldehyde, cyanothio acetamide,
1–(butenyl)pyrrolidine. Compound (39) reacted with some alkyl halides yielding 2–alkylsulfanyl nicotinonitriles (40)106, scheme 41. 12– The
one‐pot multicomponent condensation of malononitrile, 4‐methyl–pentan‐2‐one, aryl aldehyde, and ammonium acetate in ethanol yielded
the 2‐amino‐5‐isopropyl‐4‐(4‐aryl)‐6‐methyl nicotinonitriles (41 a–f), which exhibited weak antioxidant activity107,
scheme 42. 1.3.3. Catalysis mediated Synthesis of nicotinonitriles 1– The ammoxidation of 3–picoline to 3–nicotinonitrile (42) was induced by the
influence of industrially synthesized and shaped vanadium phosphate... Show more content on Helpwriting.net ...
L. Zhu et. al., reported the synthesis of new derivatives of 4–aryl–3,5–dicyano–2,6–di(3′–indolyl)pyridine (50) and polysubstituted
(3′–indolyl)pyrazolo[3,4–b]pyridine and (3′–indolyl)benzo[h]quinolines (51) via a one–pot multicomponent reaction of aromatic aldehydes,
3–cyanoacetyl indoles, and ammonium acetate employing the microwave irradiation as an energy source and ethylene glycol as a solvent,115,116
scheme 50. 2– A series of 4–aryl–6–(indol–3–yl)–2,2–bipyridine–5–carbonitrile derivatives (52) were synthesized within shorter reaction time and high
product yield via a one–pot multicomponent reaction of aromatic aldehydes, 3–(cyanoacetyl)indole, and 2–acetyl pyridine in ammonium acetate by
microwave irradiation in solvent–free condition. The same conditions were applied for the synthesis of anther series of di(indol–3–yl)–diaryl
bipyridine–dicarbonitrile derivatives (53a–e) using cinnamils, 3–cyanoacetyl indole and ammonium acetate117, scheme
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What Is Amlodipine Impurity?
AmlodipineImpurity–D3–ethyl 5–methyl 2–((2–aminoethoxy)methyl)–4–(2–chlorophenyl)–6–methylpyridine–3,5–dicarboxylate
AmlodipineImpurity–Ediethyl 2–((2–aminoethoxy)methyl)–4–(2–chlorophenyl)–1,4–dihydro–6–methylpyridine–3,5–dicarboxylate
AmlodipineImpurity–Fdimethyl 2–((2–aminoethoxy)methyl)–4–(2–chlorophenyl)–1,4–dihydro–6–methylpyridine–3,5–dicarboxylate
AmlodipineImpurity–I3–ethyl 5–methyl 2–((2–aminoethoxy)methyl)–4–(4–chlorophenyl)–1,4–dihydro–6–methylpyridine–3,5–dicarboxylate
Aripiprazolen–oxide7–{4–[4–(2,3–dichlorophenyl)piperazin–1–yl]butoxy–n–oxide}–3,4–dihydroquinolin–2(1H)–one.
AspartaneImpurity–A2–(5–benzyl–3,6–dioxopiperazin–2–yl)acetic acid.
AtenololImpurity–A2–(4–hydroxyphenyl)acetamide
AtenololImpurity–B2–(4–((oxiran–2–yl)methoxy)phenyl)acetamide ... Show more content on Helpwriting.net ...
Memantine1–chloro–3,5–Dimethyl Adamantane1–chloro–3,5–dimethyladamantane
Memantine1–Hydroxy–3,5–Dimethyl Admanatane3,5–dimethyladamantan–1–ol.
MemantineImpurity–D1–Methyl Adamanatane
MemantineImpurity–E1,3,5–Trimethyl adamentine
MemantineN–Formyl memantine1–formyl memantine
Memantine1–hydroxy 3,5–dimethyl adamantane1–hydroxy 3,5–dimethyl adamantane
MetamizoleAcetyl metamizoleN–(2,5–dihydro–2,3–dimethyl–5–oxo–1–phenyl–1H–pyrazol–4–yl)acetamide
MetamizoleImpurity–AN–(2,5–dihydro–2,3–dimethyl–5–oxo–1–phenyl–1H–pyrazol–4–yl)formamide
MetamizoleImpurity–C
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Dual ACC1 / ACC2 Inhibition
A general trend in dual ACC1/ACC2 inhibition was often encountered among the 125 compounds tested: good
ACC1 inhibition was linked to good ACC2 inhibition.4 The same group elaborated on this study by examining the structure–activity relationship (SAR)
for the pyrazole part and the substitution at position 9 of the 1,9–diazaspiro[5.5]– undecane. In this study, additional pharmacokinetics were studied
along with the IC50 values for ACC1 and ACC2, such as the lipophilic ligand efficiency (LipE), measured lipophilicity (ElogD), human liver
microsomal incubation
(HLM), and passive permeability (Papp) in Ralph Russ
canine kidney cells.6 1,9–Diazaspiro[5.5]undecan–2–one 1c
(Fig. 4) was selected for a SAR study of the effects of ... Show more content on Helpwriting.net ...
The downside was the poor Papp value obtained for compound
1h when compared to compound 1g. Compound 1i showed reasonable LipE values and diminished ACC inhibition (74 and 29 nM for ACC1 and
ACC2, respectively), but a greatly increased Papp value of 9.7 (Г—10–6 cm/s) vs 0.8 for compound 1h. Based on these results, a further SAR study
was performed by using isoquinolines and quinolines as
Figure 4. Compounds used for studying the SAR for ACC inhibition with respect to the substitution at position 9 of the 1,9–diazaspiro–
[5.5]undecane ring system.
N
H
N
c Me
Me
N
H
N
d Cl
N
H
N
e CF3
H
N
f Cl
H
N
g Cl
N
N
H
Cl
N
OMe N OMe
N
N NHMe
h i j
OMe
N
N NHPr
NHMek l m n
N NMe2 o N R
O
NHN t–BuN O
N
O
NH
N
H
N
O
N
N
i–Pr
1a o 2
N
H
N
N N
H
a b
R =
Chemistry of Heterocyclic Compounds 2017, 53(8), 827–845
830
substituents (compounds 1j–o). The development of amino– substituted species 1l–o did result in improved thermo– dynamic solubility at pH 1.2 with
a factor up to 10 when compared to compounds 1j,k. The Papp values of com– pounds 1l,m were as bad as those of compound 1h. Efforts to improve
Papp by increasing the alkylation on the amine led to compounds 1n,o exhibiting better Papp than com– pounds 1l,m. The Papp values of compounds
1n,o were still lower than those obtained for compounds 1j,k and, in addition, HLM clearance significantly worsened. Com– pounds 1j,k were chosen
for in vivo examination of their
... Get more on HelpWriting.net ...
Malaria Is A Parasite That Has Been Impacting The World...
Malaria is a parasite that has been impacting the world for the past couple of centuries. The illness associated with malaria gives intense fevers,
chills, terrible headaches, muscle pains and can be deadly if not treated properly. Although overall malaria cases have decreased from 262 million in
2000 to 214 million in 2015, it is still an issue to be concerned about today.1 There have been developments of a vaccine against this parasite, but the
parasite has adapted to the vaccine and developed a resistance to it, thus rendering it ineffective. The p. falciparum and p. vivax strains of malaria is
what is causing problems as these resistant strains have popped up in much of Asia and Africa and a couple of countries in South America.1 This can
potentially be a problem for the military and more specifically the Air Force as multiple countries where the Air Force deploys are infected with these
resistant strains of malaria. It can be seen through the background and history of the fight against this parasite that the chemistry behind an antimalarial
vaccine is important to the Air Force.
The illness associated with the malaria parasite was first thought to be a result of poisonous mists drifting from marshes hence its name meaning "bad
air" in Italian. Of course it was unbeknownst back then that it was actually caused by the female anopheles mosquito which tends to live near still
water such as marshes.2 Although it was unknown what actually caused the symptoms of malaria,
... Get more on HelpWriting.net ...
The Role of Infections and Diseases in the Evolution of...
Haldane's hypothesis which states that there is a role of infections or diseases as a driving force in the evolution of Metazoans is simply put as
infection is a selective in the evolution of Metazoans and essential for the survival of certain populations. Malaria represents one of the most important
selective factors affecting human populations. There are several inherited diseases of red blood cells that lead to resistance at the erythrocytic stage.
О±–Spectrin Hereditary Elliptocytosis
Hereditary elliptocytosis is a heterogeneous group of red–cell disorders characterized morphologically by oval–shaped erythrocytes (Gallagher, 2005).
Ovalocytosis is an uncommon variant of hereditary elliptocytosis (Gallagher, 2005). It is caused by heterozygosity for a 27–base pair deletion in the
gene encoding the erythrocyte membrane protein band 3 (SLC4A1∆27) (Williams, 2006) on chromosome 17 (Jarolim et al., 1991). A mutation
results in impaired function and gross skeletal disruption of the membrane skeleton of the erythrocyte (Coetzer et al., 1990). It confers highly specific
protection against cerebral malaria by maintaining similar parasitemia levels (Coetzer et al., 1990). The heterozygotic form is asymptotic (Coetzer et
al., 1990). Ovalocytic erythrocytes are very rigid and relatively resistant to invasion by various strains of malarial parasites (Coetzer et al., 1990).
There are four О±–spectrin mutations namely alpha 1/74, alpha 1/46, alpha 1/65 and alpha 1/61 (Coetzer et al.,
... Get more on HelpWriting.net ...
Research Paper On Pyrrolo
5.1. Introduction to Pyrrolo[1,2–a]quinoline
The chemistry of fused nitrogen heterocycles is very important because of their occurrence in numerous natural products and their versatile applications
in the pharmaceutical industry and materials science 1. Among various synthetic approaches for fused nitrogen heterocycles, pyrrolo[1,2–a]quinolines
and their oxidized and reduced forms are widespread among natural products and biologically active pharmaceuticals 2. Moreover, the skeleton of
pyrrolo[1,2–a]quinoline exists in many biologically active natural alkaloids such as gephyrotoxin (Fig. 5.1), which is a substituted
perhydropyrrolo[1,2–a]quinoline that was isolated by Daly and co–workers in 1977 from secretions of the frog Dendrobates histrionics 3 Moreover, the
isolation of gephyrotoxin a natural alkaloid with pyrrolo[1,2a]quinoline skeleton, which was subjected to numerous studies to investigate its biological
activity and has been a target for total synthesis 4.
Scheme 1. A few examples of pyrrolo[1,2–a]quinoline–containing natural products and pharmaceuticals.
Pyrrolo[1,2–a]quinoline (Fig 5.2) and synthesis of its derivatives were reviewed in 2003 by El–Sayed and El–Sayed 5. In literature, new methods or the
... Show more content on Helpwriting.net ...
An efficient method for the synthesis of fourteen novel diversified pyrrolo[1,2–a]quinoline derivatives has been described using
4–(1,3–dioxolan–2–yl)quinoline and different phenacyl bromides in acetone and followed by reacting with different acetylenes in DMF/K2CO3. The
structure of the newly synthesized compounds was determined by IR, 1H NMR, 13C NMR, mass spectrometry and elemental analysis. The in vitro
antioxidant activity revealed that, among all the tested compounds 5n has exhibited maximum scavenging activity with ABTS. The compound 5b has
showed good antiproliferative activity as good inhibitor of EGFR tyrosine
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Tattoos Research
Tattoos have a history that extends far back into the furthest reaches of time. For millennia tattoos have been used to help differentiate members of
tribes and regions and even of religions. But the concept of tattooing did not catch on in the Western world until 18th century explorers discovered
"tatau" in Polynesia; a technique that became popular among European sailors and then spread to the general populace of Western societies.
Tattoos are made by inserting indelible ink into the skin's dermis layer in order to change the skin's pigmentation for (usually) decorative reasons. In
some places and times tattoos were created by hand–tapping the ink into the skin. This could be done with sharpened sticks, bones or any sufficiently
sharp object. More modern times have ... Show more content on Helpwriting.net ...
The tattoo artist uses a stencil to draw the design onto the skin, and then outlines it with a single–tipped needle and thin ink. Shading is then done using
a thicker ink and a variety of needles and color can be applied, this is usually done more than once to ensure even coloring.
With the advent of computers to produce high quality tattoo flashes, the improvements in tattoo designs have been quite impressive, ranging from
complex single–line designs to impressively blended black and gray shading, sharply delineated colors and realistic portraiture, all of which are a far
cry from the blue and black fuzzily outlined tattoos of years gone by. And while anyone can learn to use tattoo equipment, it still takes a real artist to
create true tattoo art and the true portfolio of a real artist is not in how many tattoo flashes they have on their walls, nor even in the equipment they
have on hand, but on the number of satisfied customers they have
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The Effects Of Malaria On African Continent And Is...
Malaria is a life–threatening disease that is caused by plasmodium parasites transmitted from female mosquitos when they bite a human. The
plasmodium parasite can also be transmitted by blood products like unclean needles or unscreened blood. There are five parasite species (Plasmodium,
falciparum, P. vivax, P. ovale, and P. malariae) that causemalaria in humans, and two of these species, P. falciparum and P. vivax, are the greatest
threat (see Figure 1). The severity of malaria is based on the species of plasmodium. The symptoms people experience include chills, fever, and
sweating usually occurring within a few weeks after being bitten. In the United States, it is a very rare disease with fewer than 20,000 cases per year,
and is treatable by a medical professional. However, Sub–Saharan Africa is home to 88% of malaria cases and 90% of malaria deaths. P. falciparum is
the most prevalent parasite on the African continent and is responsible for most malaria–related deaths globally. P. vivax is more widely distributed
than P. falciparum and predominates in most countries outside of Africa. In the 1970s and 1980s, resistance of P. falciparum started in medicines, such
as chloroquine and sulfadoxine–pyrimethamine (SP). Drug resistance has been implicated in the spread of malaria to new areas and re–emergence of
malaria in areas where the disease had been eradicated. Population movement has introduced resistant parasites to areas previously free of drug
resistance. Resistance is
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Nucleophilic Reaction Lab Report
March 2017 Selective Synthesis Dispiro[indoline–3,2′–pyrrolidine–3′,3″–quinoline]
Derivatives and Spiro[imidazole–4,3′–quinoline] Derivatives via
1,3–Dipolar Cycloaddition Reaction
859
M
niv am cem
02/
On
e–3 de cycloadditio
structure 4
The target compound 7 was prepared by adding the re– ortion. The poxide for–
ave methyl
© 2016 Wiley Periodicals, Inc. nitrogen atom from sarcosine and carbonyl of isatin, 4–hydroxy–7–methoxy–2–oxo–1,2–dihydroquinoline–3–carbo for
this reaction, leading to the formed spiro
. The nucleophilic reaction between the
Moreover, the treatment of compound 9 w disulphide in the presence of dimethylsulphate g
Chemistry. The 1,3–dipolar cycloaddition reaction of azomethine ylide b with dipolarophile 3 yielded ... Show more content on Helpwriting.net ...
Anal. for C28H25N3O5 (483.18): Calcd: C
69.55, H 5.21, N 8.69%. Found: C 69.59, H 5.19, N 8.50%.
2–Amino–7′–methoxy–5–(4–methoxyphenyl)–2′H–spiro[imidazole–
4,3′–quinoline]–2′,4′ (1′H)–dione (7). A mixture of 3 (1.0 g,
3.23mmol), H2O2 (0.37mL, 30%), and ethanol (20mL) was stirred at room temperature then added guanidine nitrate (0.59 g, 4.83mmol) and aqueous
solution of KOH
(50%) (1.30mL) were stirred at 80В°C for 2 h. The ethanol was evaporated, and water (30mL) was added to the reaction mixture remainder. The
outcome product was п¬Ѓltered off, washed accurately with water. The wet product slightly still wet п¬Ѓlter cover was mixed with ethanol (10mL),
and the resulted suspension refluxed for
30min. After cooling, the precipitate was п¬Ѓltered off, washed with ethanol, and п¬Ѓnally dried.
Yellow crystals (0.35 g, 30%), mp 196–197В°C (DMF/
H2O); Rf = 0.63 [ethyl acetate: pet. ether (40:60)](1.5:4);
IR(KBr): Оі/cmпїЅ1 = 3327 (NH2), 3267 (NH), 1658 (CO),
1612 (CONH); 1H NMR (CDCl3): Оґ: 3.72 (s, 3H, OCH3– quinolone), 3.83 (s, 3H, OCH3–aromatic), 6.77–6.89 (m,
7H, aromatic–CH), 7.87 (broad s, 1H, NH, D2O exchange– able), 9.83 (broad s, 2H, NH2, D2O exchangeable);
... Get more on HelpWriting.net ...
The Most First Time Of Zopf
The very first time, Zopf was described the genus Rhodococcus in 1981 and then redefined in 1977 to accommodate a number of strains that
resembled but did not belong to the genera Corynebacterium, Mycobacterium and Nocardia.1, 2 Thereafter, considerable changes were made to the
classification of the genus. Some species have been combined, some reclassified in new genera and new species have also been described.1 at present
there are over 40 species classified under the genus Rhodococcus.3–4
The genus Rhodococcus are aerobic, GC– rich nonsporulating, non motile Gram–Positive bacteria which also contain mycolic acids in their cell
envelope.5–7 The cell wall of rhodococci are chemotype IV, means the peptidoglycan is mesodiaminopimelic acid... Show more content on
Helpwriting.net ...
For instance, the production of acrylamide from acrylonitrile by using Rhodococcus rhodochrous J1.13 Rhodococci present a unique enzymatic
capabilities, for instance Rhodococcus erythropolis produce large number of enzymes that allow them to undergo the reactions like bioconversation
and biodegradations.14
Biosurfactants and bioflocculants
Rhodococci have the ability to produce surfactant molecules, which contain strong hydrophilic and hydrophobic groups and also migrate to interfaces
between oil and aqueous phases. Some biosurfactants, including some Rhodococcus produced surfactants that are more efficient, more degradable and
less toxic than synthetic surfactants. The relevance of surfactants to biodegradation of pollutants is threefold; the cellular surfactants cause adherence
of rhodococci to hydrophobic phases in two phases and surfactants lower the interfacial tension between the phases, making it easier for hydrophobic
compounds to enter the cell. At the same time extracellular surfactants disperse hydrophobic compounds that increase the surface area for the
attachment of mycolic acids.1
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INTRODUCTION:- HISTORICAL BACKGROUND OF ANTIHYPERTENSIVE...
INTRODUCTION:– HISTORICAL BACKGROUND OF ANTIHYPERTENSIVE THERAPY Antihypertensive therapy with the conventional drugs
such as thiazide diuretics,beta –adrenoreceptor antagonists and Calcium channel antagonist (CCA ) based regimens can reduce the risk of stroke and
other cardiovascular events. The drugs used as first line therapy in both younger and elderly patients include the conventional drugs such as diuretics,
CCA or ACE inhibitors based regimens[6][7] ACE inhibitors such as Captopril and enalapril are used clinically for the treatment of hypertension and
congestive heart failure(CHF). Despite the fact that ACE inhibitors have met with a high degree of success, ACE is a nonspecific protease responsible
for degradation of bradykinin... Show more content on Helpwriting.net ...
So we got an idea to synthesize some new AT1 receptor antagonists which do not have these side effects. RENIN ANGIOTENSIN ALDOSTERONE
SYSTEM:– [13] The renin angiotensin system is one of the powerful regulators of blood pressure and volume homeostatis. Renin is a proleolytic
enzyme which is produced in the juxtaglomerular apparatus of the kidney. It acts on the angiotensinogen which is a–globulin produced by the liver.
Then there is a formation of Angiotensin 1 (decapeptide) Asp–Arg–Val–Tyr–Ile–His–Pro–Phe–His–Leu. Ang1 has little biological activity. Then
Angiotensin is produced when there is removal of the C –terminal dipeptide Histidyleucine from Ang 1 by the action of metalloprotease enzyme ACE
(Angiotensin converting enzyme) mainly present in lungs and Angiotensin II (1–8) is produced which is an octapeptide in regulating the
mineralocorticoids, it induces the sodium and water retention in the body. ANGIOTENSIN II RECEPTOR BLOCKERS:– Angiotensin II receptor
blockers (ARBs) (eg, valsartan, losartan, candesartan, telmisartan, tolmesartan, and irbesartan) act by selectively blocking the AT1 receptor, thereby
directly blocking the vasoconstrictor and growth effects of Ang II.[16] Selective blockade of the AT1 receptor has additional cardiovascular benefits
resulting in vasodilation, growth
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Air Pollution Is An Unavoidable Mixture Of Substances That...
Air pollution is an unavoidable mixture of substances that we breathe in. There is no way to escape air pollution nowadays since it can be
encountered indoors as well as outdoors. The type of pollution we breathe in can be divided between indoor and outdoor by the different types of air
pollution that are released in these environments. Fine particles such as burning fossil fuels (such that come from traffic and energy production),
tobacco smoke, and chemical vapors are found in the air breathed in from outdoors, while solvents (such as found in household cleaners and products),
mold, and carbon monoxide are sadly breathed in from within homes and businesses on a daily basis.
There is no question to anyone's mind that these air pollutants cause harmful effects to one's health. Studies have been conducted to link air pollution to
the hundreds of ailments that many men, women and children have suffered over the years. Cardiovascular and respiratory illnesses are without a
doubt caused by air pollution as studies have shown. Today there are studies showing thatAutism is linked to air pollution. The purpose of this paper is
a review of the current state of knowledge on air pollution and whether it plays a role in children developing autism.
Autism is a disability that impairs the normal brain development in children. It causes deficits in their verbal and non–verbal communication, social
interaction, and play. Girls are more likely to show severe characteristics of the
... Get more on HelpWriting.net ...
Synthesis Of Pi3k Inhibitors
To start with, the synthesis of class I and class III phosphoinositide 3–kinase inhibitors has become a much–needed research process. Creating and
modifying the PI3K inhibitors through the addition and elimination of organic functional groups or amino acids has allowed scientists to find the best
way in attacking the irregularities formed in the body. Plenty of class I PI3K inhibitors– like those seen in Figure 3– have been identified and modified
for therapeutic means. For example, GDC–0941 and BKM–120 are both inhibitors that are being considered as possible clinical trial candidates [2].
Other inhibitors have also been developed for specific PI3K isoforms which helps to highlight the usefulness of the PI3K pathways [2]. To get a better...
Show more content on Helpwriting.net ...
In the studies being done, scientists realized that the BKM–120 inhibitor not only affects the PI3K/PKB/mTOR pathway, but the microtubule synthesis
pathway, as well [5]. This dual activity found in the BMK–120 inhibitor was due to the structure of the inhibitor; Figure 5 illustrates how these two
functions are possible (a) and what the ratio of microtubule inhibition and PI3K inhibition are in the cell (b) [5]. Through extensive studies on the
BMK–120 inhibitor and other similar compound structures, researchers, like Bohancker et al., have been able to identify key structural components for
the two activities. The Bohancker et al. found that additional nitrogen in the core of the molecule could help remove the tubulin inhibition, as well as,
less symmetry in the BMK–120 overall structure [5]. In general, the research being done in these two examples, and the many other inhibitor synthesis
experiments, show how the creation and modification of the phosphoinositide 3–kinases inhibitors is a huge part PI3K studies. From these
developments, scientists can get a better sense of how the inhibitors will work in cells and treating diseases. Though the synthesis of phosphoinositide
3–kinase inhibitors is necessary for advancements in this field, research on how efficient and effective these inhibitors are is just as imperative. Many
assays have been developed to study the effectiveness of PI3Ks– mainly through the quantifying of kinase
... Get more on HelpWriting.net ...
Biodegradation of Hydrocarbons from Crude Oil by...
Biodegradation of Hydrocarbons from Crude Oil by Pseudomonas putida
A Project done under the guidance of
Dr. K. Bharathi Department of Biotechnology.
Submitted to the faculty
Of
Department of Biotechnology
National Institute Of Technology, Warangal (A.P)
Submitted By Febin P. Nalpady, Anzal Rahman, Shruti Sharma, Sindhuja Nandiraju, Giraboina Kranthi Kumar NATIONAL INSTITUTE OF
TECHNOLOGY
WARANGAL (A.P)
(DEEMED UNIVERSITY) 2010–2011 ... Show more content on Helpwriting.net ...
2.Introduction
In quantitative terms, crude oil is one of the most important organic pollutants in marine environment and it has been estimated that worldwide
somewhere between 1.7– 8.8Г—106 tons of petroleum hydrocarbons impact marine waters and estuaries annually. Reports have been appearing since
last three decades on the biodegradability of crude oil by bacteria which can use hydrocarbons as source of carbon and energy. A way to mitigate the
effects of oil spills is bioremediation. 2.1 Bioremediation It is a process by which chemical substances are degraded by bacteria and other
microorganisms. The use of these microorganisms has been successfully applied for the treatment of waste and wastewater in controlled systems.
Several research studies have recently been performed to investigate the use of bioremediation for oil–spill cleanup in seawater, freshwater and
terrestrial areas. The technique has been found to have a potential for broad applications in terrestrial and freshwater environments for treating soils and
sediments contaminated with oil and other substances, as well as for coastal environments impacted by oil spills. Water is a more sensitive medium
than soil and requires different remediation techniques. Spills to surface water are easier to clean up than spills to groundwater, for obvious reasons. It
is not only much harder to see the extent of the contamination, but also to remove the source of the contamination as, for
... Get more on HelpWriting.net ...
Advantages And Disadvantages Of Benzofuran
INTRODUCTION: The metal chelates of various ligands play pivotal role in many important medicinal applications. They also useful for metal
extraction and detection. The present aspect is context to the novel heterocyclic ligand containing .pharmaceutica active segments like benzofuran,
1,3,4–oxadiazoe and p–amino salicylic acid as ligand. So the literbture review is as follow:
LITERATURE REVIEW:Chelating agents, because of their metal specificity or selectivity, can function as good flotaids and selective flocculants. In
addition to the metal selectivity, chelating agents offer certain advantages over conventional mineral processing reagents even from the synthesis point
of view. With the major donor .atoms–S, N, 0 and, to some extent, P–numerous possibilities exist to tailor make reagents for specific applications.[1–3]
For polymers the backbone offers further possibilities for the incorporation of the required properties. In general, the choice of a chelating agent or a
group is made on the basis of its function in well–known analytical metal separations. Such a choice is limited in that the number of well–known ...
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Objectives:
a.The objectives of the proposed work are To synthesis : and characterize benzofuran–1–;3,4–oxadiazole–p–amno salicylic acid ligands.
b.To prepare the metal, chelates of above ligands and stheir characterization
WORK PLAN:
Following work will be carry out
Synthesis of Benzofuran–1,3,4–oxadiazole derivative
The Mannich reaction of above derivative with p–aminosalicylic acid
Characterization of all the derivatives.
The transition metal chelates preparation and characterization by metal:ligand ratio, spectral study and magnetic properties.
Testing of microbicidal
... Get more on HelpWriting.net ...
Different Definitions Of Key Terms
Definitions of key terms
However, looking at the conceptual perspective, Colwell, R. R., and J. D. Walker (1977, cited in Aniefiok E. Ite1, et al., 2013: p 78
–79) defines oil as
follows:
"Oil is a naturally stirring multipart mixture made up primarily of hydrocarbon mixtures and normally contains substantial quantities of nitrogen,
sulphur, and oxygen together with smaller amounts of nickel, vanadium, and numerous components. Oil compounds can occur in solid form as asphalt,
liquid form as crude oil and/or gaseous form as natural gas. Petroleum hydrocarbons could be divided into four classes: saturates (pentane, hexadecane,
octacosane, cyclohexane), aromatics (naphthalene, phenanthrene, benzene, pyrene), asphaltenes (phenols, fatty acids, ketones, esters, and porphyrins),
and resins (pyridines, quinolines, carbazoles, sulfoxides and amides)". : P 78–79
Natural gas is the world 's third major energy source, estimated at 21% of total prime energy usage (www.indexmundi.com/commodities/market). On
the other hand, environmental risks are consequences that result from oil exploration to the communities (e.g. workers, consumers and local people).
CHAPTER TWO
LITERATURE REVIEW
2.0 Introduction
This chapter focuses on what other scholars have written about risks associated with oil and gas exploration, drilling and extraction in various parts of
the World. The chapter is structured in accordance with the objectives of the study, that is, to assess the
... Get more on HelpWriting.net ...
Symptoms And Treatment Of Alzheimer 's Disease
Introduction The neurodegenerative disorder Alzheimer's Disease (AD) is currently the most common cause of dementia and affects millions of
people around the world.В№ There are multiple risk factors associated with AD, including genetic factors, hypertension, diet and most significantly,
age. Individuals over the age of 65 are most vulnerable to the disease and at this point, the risk increases every 5 years.В№ Alzheimer's Disease was
first described over 100 years ago by Alois Alzheimer in Germany, characterising the first case with memory impairments and the presence of
neuropathological plaques and tangles, which today, are major indications of the disease.ВІ Progressive memory loss is the clinical trademark of AD
but eventually, cognitive function also deteriorates.Ві The neuropathological trademarks of AD involve the accumulation of ОІ amyloid (AОІ) proteins
expressed as plaques and the phosphorylation of tau proteins expressed as neurofibrillary tangles.Ві The formation of these plaques and tangles are
estimated to begin 20 years before clinical symptoms arise.ВІ MRI studies have shown the association of AD with hippocampal atrophy, however, it
remains difficult to distinguish from other forms of dementia.вЃґ However, this pathology is also known to be present without the impairment of
cognitive function.вЃµ Recently, there has been a number of studies investigating this incongruity between pathology and cognition, all of which
reported similar dissonance, remarkably in older
... Get more on HelpWriting.net ...

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Effective Malaria Treatment Is Fraught With Challenges

  • 1. Effective Malaria Treatment Is Fraught With Challenges Effective malaria treatment is fraught with challenges. Resistance is seemingly around the corner for every previously superlative drug, while being deeply entrenched among those medications that a few decades ago were vital to chemotherapy. For artemisinin, the first signs of resistance were observed in a 2008 study of parasite clearance times following monotherapy with artesunate. Clearance was slower among patients from the Eastern Thai–Cambodian border than that of patients from the Thai–Myanmar border to the West (Dondorp et al., 2009). Though an alarming fact on its own, when coupled with the proportional increase of such slow–clearing infections from 0.6% in 2001 to 20% in 2010 with rates approaching 42% in Cambodia one must conclude that there is cause for alarm (Flannery et al., 2013). Resistance is not only emerging but also spreading. Now more than ever we have need of new medicines as well as new approaches for producing those medicines. The link to plant physiology among Plasmodium spp. is basically irrefutable and imperatively needs further investigating. By elucidating essential biosynthetic pathways behind such compounds like abscisic acid, we can find hitherto unknown targets as well as broaden our knowledge of the evasion mechanisms that are at the disposal of our protozoan foes. Evasion is the primary response of malaria in response to the immune system's efforts and this tactic appears to have been extended to one of the most powerful drugs we have. ... Get more on HelpWriting.net ...
  • 2. Verapamil Research Paper Verapamil has 4 different kind of dosage form which orally in tablet, tablet controlled release, capsule extended release and injection form. The ingredient for making tablet has pharmacological action is verapamil hydrochloride. Each tablet oral contains 40mg, 80mg, 120mg and 160 mg of the active ingredient. The other excipients are magnesium stearate, propylene glycol, sunset yellow aluminium lake, quinoline yellow aluminium lake, titanium dioxide, microcrystalline cellulose, hydroxypropylcellulose and methylhydroxypropylcellulose. Beware using sunset yellow aluminum lake because it can cause allergic reactions. The steady state has to be controlled to obtain optimal therapeutic effect and also patient compliance needs to be considered. Therefore, controlled... Show more content on Helpwriting.net ... Due to HPMC is a pH–independent polymer, it sustain the drug release by hydrating to form a gel layer at the surface of the tablet. Sodium alginate is a pH–dependent, when exposed to acidic in stomach; it will convert to insoluble alginic acid. By the way, the type and amount of polymer affected the release of drug. For both forms of tablets usually should be stored in tight, light–resistance container or amber glass at 15–25 oc. The shelf life is three years from the date of manufacturing. For capsule extended release oral contains 100mg, 120mg, 180mg, 200mg, 240mg, 300mg and 360mg of the active ingredient. These forms using the diffusion delivery system which are consists of controlled–release coated pellets enclosed in a hard gelatin capsule. Polymers can be using both water soluble and water–insoluble polymers. When exposed to water in GI tract, the soluble polymer will slowly dissolves, allow the drug to diffuse while the insoluble polymer act as barrier maintaining controlled release of the drug into GI tract. It should be stored in tight light–closed container at room temperature ... Get more on HelpWriting.net ...
  • 3. Acts : Discussion : Artemisinin-Based Combination Therapies Discussion Artemisinin–based combination therapies (ACTs) are currently considered gold standard in the management of uncomplicated malaria. For the liver stages, primaquine is the only drug approved to eliminate hypnozoites. Resistance against existing antimalarials is well documented, and troubling due to the emerging resistance to artemisinins. Therefore, a rising incidence of drug resistance requires the development new drugs, with novel disease targeting strategies. Moreover, the challenge is to develop innovative drugs that demostrate (i) faster onset and longer duration of drug action, (ii) safe for children and pregnant women, and (iii) ideally be amenable to a single–dose administration. Following are brief descriptions of such ... Show more content on Helpwriting.net ... Ferroquine, unlike chloroquine, accumulates in the digestive vacuole of the chloroquine resistant parasites, enabling P. falciparum chloroquine resistance transporter, PfCRT inhibition. [6] 3.Amodiaquine is also active against most chloroquine resistant strains, however, two reactive metabolites are formed, namely imine and aldehyde, and are the likely cause of the hepatotoxicity and agranulocytosis, respectively. [7] 4.N–tert–Butyl isoquine (GSK369796) was designed to avoid the formation of quinone imines, and has entered Phase I studies. It is potent in vitro, including in the chloroquine resistant strain K1 (EC50 = 13 nM) and is active in vivo with an ED50 = 3.8 mg/kg/day, thus being comparable to amodiaquine. In spite of the excellent exposures and near quantitative oral bioavailabilities in animal models, its development was discontinued due to exposures insufficient to demonstrate drug safety superior to chloroquine. [8] 5.In an effort to select the next generation of quinoline methanol derivatives that could serve as a replacement for mefloquine, the Walter Reed Army Institute of Research screened for analogs with a lower brain penetration, and identified WR621308, which has a substantially lower permeability across MDCK cell monolayers than mefloquine, suggesting lower brain exposures. [9] 6.Cycloguanil and pyrimethamine demonstrate inhibition of dihydrofolate reductase (DHFR). ... Get more on HelpWriting.net ...
  • 4. Target For Schizophrenia Essay PDE10A–A target for schizophrenia? Phosphodiesterases (PDEs) are a class of enzymes, which are responsible for the breakdown of phosphodiester bonds, specifically hydrolysing cyclic nucleotides, like the secondary messenger molecules cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in the striatal region of the brain.1 Via their control of both cAMP and cGMP in the cell, PDEs contribute to cell signalling making them potentially important drug targets.2 This enzyme class consists of 11 different families, PDE1 to PDE11, which vary in sequence homology, domain architecture and sequence homology.1 PDE10A is a PDE of current interest as a possible target to treat neurological diseases such as Schizophrenia and... Show more content on Helpwriting.net ... The active site contains residues that form complementary interactions to MP–10 (Figure 3B), there are several hydrophobic interactions, from certain amino acid residues in the active site of PDE10A to the MP–10 inhibitor, in particularly the quinoline and pyridine moieties. There are also two hydrogen bonds between the active site and MP–10, which is via the phenol group (donor) on the tyrosine (Tyr683) residue to the nitrogen (acceptor) in the quinoline moiety and to the ether oxygen (acceptor) within MP–10.6 Chemoproteomics Demonstrates Target Engagement and Exquisite Selectivity of the Clinical Phosphodiesterase 10A Inhibitor MP–10 in Its Native Environment The study, by SchuМ€lke et al. aimed to provide information that enables further development of chemical biology probes for important classes of enzymes, particularly focussing on developing a chemical probe for the PDE10A enzyme. To characterise the target engagement of MP–10, SchuМ€lke et al. designed a photoaffinity probe for PDE10A which contained a linker attached to the PDE10A recognition element (Figure 4), so that a reporter group could be introduced without effecting the proteins activity. The group decided, via studying the cocrystal structure, that the pyrazole nitrogen would be the best site for linker attachment as it is unsubstituted and a relatively synthetically accessible point of modification. Adding to ... Get more on HelpWriting.net ...
  • 5. The Epidemic Of Vibrio Cholera Vibrio cholera is a gram negative rod shaped bacteria which colonises the human gut causing acute diarrheal disease and leads to frequent epidemics around the world. In 2014 190, 549 cholera cases were reported to the World Health Organisation (Global Health Observatory Data 2014) , however the true number is likely to be far higher as there are many greatly affected locations which have poor or nonexistent data. Vibrio cholera is currently treated by the use of oral antibiotics coupled with rehydration therapy however the bacteria are now developing resistance and new treatments must be produced in order to prevent further epidemics and unnecessary deaths. This essay will discuss the pathogenesis of Vibrio cholera bacteria along with antibiotic treatment of cholera and its methods of antibiotic resistance. There are twenty known groups of the vibrio cholera bacteria however, group V.cholerae 01 and group V.cholerae 0139 only are capable of causing epidemics. The main causes for the spread of these strains to cause epidemics are transmission via drinking untreated water from a water source with similar conditions to the where the organism would naturally grow, or via eating or drinking produce contaminated by the faeces of infected people. Once ingested pathogenesis occurs. The bacteria enter the human gut and begin to colonise the small intestine. Their flagella provide motility and digestive enzymes such as mucinase, a mucolytic enzyme which depolymerises mucus, allow ... Get more on HelpWriting.net ...
  • 6. Hydrazino-Spengler Essay 8.Hydrazino–Pictet–Spengler ligation reaction = In this reaction, the aliphatic and aromatic hydrazines are used as a substrate to undergo pictet–spengler reaction with aldehydic and ketonic group. As described in the above category 7, the various substrates are used for ligation with aldehydic and ketonic groups of the proteins, P. Agarwal and research group developed the Hydrazino–Pictet–Spengler(HIPS) ligation reaction so that the stable protein conjugates can be developed . This strategy can be used in the development of a prodrug delivery system. The advantage of this scheme over the other oxime and hydrazone ligations is that the ligation proceeds very fast near the neutral pH(that is the pH of the normal physiological body) and the product of the HIPS ligation is showing very long stability in human plasma (approx 5 days) as compared to that of oxime–linked conjugate (approx 1 day). This was monitered by protein–fluorophore conjugates by ELISA(42). Scheme 18. Overview of the Hydrazino–Pictet–Spengler reaction. A) In reaction with a small molecule and B) protein aldehydes, a Cв€’C bond (highlighted in red) is formed between the indole and the aldehyde of interest ... Show more content on Helpwriting.net ... It is a very important reaction for the synthesis of the larged fused heterocyclic compounds. Researchers have developed a lot of series of fused heterocycles and analyzed them for their physiological and therapeutic effect. Many new drugs are there in the market that are being synthesised from this valuable and novel reaction. The researchers have also undergone experiments regarding the effect of using various types of substrates, solvent system, catalyts, temperature and many other parameters on the rate and yield of the reaction. Still a lot of research work is being going on to bring the modifications in the reations. In short, this reaction has a bright future aspects in terms of research ... Get more on HelpWriting.net ...
  • 7. Organic Food Research Papers Food directly affects to human health; it supplies energy for human activities. Now, choosing good foods for family becomes a hard problem with many households when people hear about the toxic ingredients in food every day. The diseases, which have been linked to food poisoning, are increasing day by day. The development of new technology analyzed the nutrient elements, and figured out the risks of poisonous elements in food. The scientists researched a new farming method called organic farming method that is producing the best quality food for every person. Nowadays, organic food has become a familiar term with many people. People should consume organic food because it reduces health risks, tastes great, protects the environment, and ... Show more content on Helpwriting.net ... For instance, the effect on cells is up to four times when Brilliant Blue and MSG are combined. It will go up to seven times when Quinoline Yellow and Aspartame are combined together (Lee par. 6). The reason of diarrhea is from remaining toxic elements, which cannot be cleaned by rinsing. Moreover, organic foods have more nutritional elements. Those are essential ingredients, which enhance people's health. According to the Organic Consumers Association, organic food has 25% more nutrition in terms of vitamins and minerals than products derived from industrial agriculture. Organic products have higher level of beta–carotene, vitamin A, D, E, essential acids, and essential minerals ("Why We" par. 1 –2). Furthermore, organic farming method also protects the farmers and the pickers who are working and contacting with pesticides everyday on the farm. The consumers protect the farmers indirectly, and protect themselves directly because organic food does not contain pesticides. In 2007, according to the United States Environmental Protection Agency data, the amount of pesticide active ingredient used in farming in the U.S. is 1,133 million pounds (3). It is true that the remaining pesticides can be removed after washing in some kind of fruit and veggies, but it is only a small proportion. The remaining pesticides in non–organic food cannot be removed after washing especially in thinner skin fruit such as strawberries, ... Get more on HelpWriting.net ...
  • 8. Coal Tar Production Essays Production The complete process of coal tar production is shown in Figure 1. The coal tar is produced by carbonization of coal. In this process, the coal is heated at 900–1100 ВєC and the evolved vapors are condensed to form liquid, from which ammonia is removed to obtain a black viscous crude coal tar. The composition of tar so obtained depends upon the origin and composition of starting material used viz. bituminous (soft) coal, anthracite (hard) (Arnold 1997, Thami 2002). Crude coal tar can be further purified using various techniques viz. solvent extraction, fractional distillation or coloum chromatography. The extraction of crude coal tar with alcohol containing 5% w/w Tween 80 produces Liquor carbonis detergens (LCD). Similarly, the... Show more content on Helpwriting.net ... Characterization It is most commonly analyzed with either Liquid Chromatography having Ultraviolet/ Fluorescence detection (HPLC/UV, HPLC/FD) or Gas Chromatography coupled with Mass Spectroscopy (GS–MS) (EPA 1994; Litofsky1999; Gruber et. al., 1970). Both the techniques offer high sensitivity and selectivity. However, the high cost of equipment and long run time, especially for LC, are the barriers for their utilization in routine analysis. The other techniques which can be been explored to characterize the coal tar are Spectrofluorimetry (Li 1994, Raza 2012,), Nuclear magnetic resonance (NMR) and Fourier Transform Infrared Spectroscopy (FTIR) (Nelson 1996, Cerny 1991). Pharmacological action Despite its long history of use and wide acceptance, the exact mechanism of action of coal tar is still elusive. Coal tar is known to posses keratolytic, anti–pruitic, anti–mitotic, and anti inflamatory activities (Paghdal, 2009);; Roelofzen 2007). The researchers have put forward many theories to explain these pharmacological actions viz. suppression of DNA synthesis, inhibition of sebum production, photosensitizing effects within the range of the ultraviolet light A (UVA) and visible light spectrum (Gruper 1971, Arnold, 1997, Thami, 2002, Everett 1961, Kaidbey 1977). The constituents that are thought to be responsible for these therapeutic dermatologic effects include the followings; (1) Acridine compounds in the ... Get more on HelpWriting.net ...
  • 9. Kill Parasites Than Chloroquine As A Weekly Prophylaxis 2.2.2.2 Amodiaquine Amodiaquine (Figure 2.3b) is another example of 4–aminoquinoline. It is similar with chloroquine, but it can more effectively kill parasites than chloroquine, as well as a weekly prophylaxis. Because of the similar structure, amodiaquine is supposed to have the same antimalarial mechanism. Hayeshi et al. [20.45] and Fley and Tilley[20.46] proved that amodiaquine can accumulate in digestive vacuole and bind to heme. Besides, an incomplete cross–resistance has been found between amodiaquine and chloroquine, this may be due to the mutation of PfCRT and PfMDR1. 2.2.3 8–Aminoquinoline 2.2.3.1 Pamaquine Pamaquine (Figure 2.5b) is an 8–aminoquinoline, synthesized based on the structure of methylene blue (Figure 2.5a). It is the first antimalarial drug that has activity against liver stage parasites, and can prevent the relapse of P. vivaxmalaria. Although pamaquine can delay the first attachment of malaria, it is an incomplete protection. So at that time, pamaquine was usually combined with quinine to treat malaria. However, pamaquine was reported with severe toxicological concerns, relating with glucose 6–phosphate dehydrogenase (G6PD) deficiency, and it is not as efficient as primaquine. Because of these problems, pamaquine is no longer used. 2.2.3.2 Primaquine In 1940s, primaquine (figure 2.5c) was first synthesized by Elderfield[wiki.2]. Although it still has side effects for G6PD deficient patients just like pamaquine, it can more efficiently treat P. ... Get more on HelpWriting.net ...
  • 10. Electrochemical And Quantum Chemical Studies Of The... Electrochemical and quantum chemical studies of the corrosion and hydrogen evolution reaction of mild steel in acid medium Rabab M. El–Sherif a,*, K. M. Zohdy b Sowmya Ramkumar c a Cairo University, Faculty of Science, Department of chemistry, Giza, 12613, Egypt b Higher Technological Institute, 10th of Ramadan City, Egypt c Department of chemistry, PSGR Krishnammal College for Women, Peelamedu, Coimbatore, India Abstract Electrochemical behavior and hydrogen evolution reaction of mild steel in sulfuric acid solutions, containing different concentrations of gamma–Aminobutyric acid (GABA) as a green inhibitor have been investigated. The electrochemical techniques included Tafel polarization and electrochemical impedance spectroscopy (EIS). The rate of both the corrosion reaction and the hydrogen evolution affected significantly by changing GABA concentrations. Polarization results showed that GABA is a mixed type inhibitor with good inhibition efficiency. Increasing the temperature led to an increase in the hydrogen evolution rate and a decrease in the total surface resistance value (RT) or the relative film thickness (1/CT) of the steel. Quantum calculation including EHOMO, ELUMO, the energy gap (?E) and the fraction of transferred electrons (?N) demonstrated the inhibition ability of GABA. The results were confirmed by surface examination using scanning electron microscopy. Adsorption of GABA on the steel surface fitted the Langmuir isotherm. Thermodynamic parameters ... Get more on HelpWriting.net ...
  • 11. Artemisinin Based Combination Therapies ( Acts ) Artemisinin–based combination therapies (ACTs) are currently considered gold standards in the management of uncomplicated malaria. For the liver stages, primaquine is the only drug approved to eliminate hypnozoites. Resistance against existing antimalarials is well documented, and troubling due to the emerging resistance to artemisinins. Therefore, a rising incidence of drug resistance requires the development new drugs, with novel disease targeting strategies. Moreover, the challenge is to develop innovative drugs that demostrate (i) faster onset and longer duration of drug action, (ii) safe for children and pregnant women, and (iii) ideally be amenable to a single–dose administration. Following are brief descriptions of such innovative... Show more content on Helpwriting.net ... 2.Ferroquine was found to be active against chloroquine– resistant strains, and is currently undergoing Phase II clinical trials. Ferroquine, unlike chloroquine, accumulates in the digestive vacuole of the chloroquine resistant parasites, enabling P. falciparum chloroquine resistance transporter, PfCRT inhibition. 3.Amodiaquine is also active against most chloroquine resistant strains, however, two reactive metabolites are formed, namely imine and aldehyde, and are the likely cause of the hepatotoxicity and agranulocytosis, respectively. 4.N–tert–Butyl isoquine (GSK369796) was designed to avoid the formation of quinone imines, and entered Phase I studies. It is potent in vitro, including in the chloroquine resistant strain K1 (EC50 = 13 nM) and is active in vivo with an ED50 = 3.8 mg/kg/day, thus being comparable to amodia– quine. In spite of the excellent exposures and near quantita– tive oral bioavailabili ties in animal models, its developmen t was discontinue d due to exposures insufficient to demonstrate drug safety superior to chloroquine. 5.In an effort to select the next generation of quinoline methanol derivatives that could serve as a replacement for mefloquine, the Walter Reed Army Institute of Research screened for analogs with a lower brain penetration, and identified WR621308, which has asubstantially lower permeability across MDCK cell monolayers than mefloquine, suggesting lower brain ... Get more on HelpWriting.net ...
  • 12. MRSA: The Role Of Antibiotic Resistance In Bacteria Lastly, but most importantly, antibiotic misuse needs to be avoided because it can lead to antibiotic resistance. Antibiotic resistance is a bacterium's ability to overcome the effects of antibiotics and to survive in the presence of them ("About" par. 1). This is what causes antibiotics to be ineffective towards some bacterial infections. When a bacteria is exposed to the same antibiotic regularly, that bacteria mutates to become antibiotic resistant. Bacteria have many mechanisms of resistance. For instance, bacteria can achieve resistance by changing the chemical structure of their cell walls, pumping the antibiotic out of their cell via pumps, and acquiring enzymes that inactivate antibiotics (Groopman 57). Since there are many ways ... Show more content on Helpwriting.net ... While this may be true in some instances, it is a very dangerous approach to antibiotic use because of the many negative effects. As stated earlier, the term "antibiotic" translates to "against life" because antibiotics are used to kill living organisms; therefore, if antibiotics are used irresponsibly and in large quantities, they can kill humans. Further, the adverse effects caused by antibiotics may have negative consequences. For example, antibiotics eliminate benign bacteria in the human colon, which allows opportunistic bacteria to take over (Sachs 191). As previously stated, this may cause many complications such as Clostridium difficile infections, diarrhea, and fatal colon inflammation (Surawicz par.1,3). C. difficile is responsible for 29,000 deaths a year (Lessa, et. al. par. 18). That number is too great to overlook. Additionally, Antibiotics can cause Klebsiella, a bacteria that has a multidrug resistant strain (Johnson 52). Furthermore, widespread antibiotic use will not cure every illness. Despite forty percent of people believing that antibiotics can cure viral infections, antibiotics are only effective against bacterial infections ("Entrenched" par. 5). Lastly, widespread antibiotic use leads to antibiotic resistance. Every year resistant bacteria are the cause of two million infections in the United States (Alic par. 2). If ... Get more on HelpWriting.net ...
  • 13. Ocular Melanoma Research Paper While researching in depth Ocular Melanoma, there has been a consistent theme persisting there is not enough research done to find a way to decrease metastasis percentage and increase survival rate. The current attempts at decreasing metastasis and increasing survival rate have stayed the same throughout the course of 4 decades. The current drug, LS2616, is being used to treat Ocular Melanoma patients, but it is used to late to feel the full impact of the drug. Research and Development laboratories are working on a faster–acting drug, but nothing has been tested on mice or released to the public. If new drugs could be created, the survival rate of Ocular Melanoma would increase drastically. History Ocular Melanoma (OM) is a deadly killer. ... Show more content on Helpwriting.net ... There are two main categories for treatment; radiation and surgery. The choice is ultimately up to the patient, but depending on the size and location of the tumor, different treatments work better. Radiation and surgery treatments have both pros and cons. " Plaque radiation therapy is the most common and effective radiation for ocular melanoma" ("Ocular Melanoma Treatment", 2016, para 4.). It can be distributed either by a machine or by a gold plaque, that resembles a lot like a tiny bottle cap. Removing the tumor surgically or removing the eye all together are the two most common surgical methods. If the tumor is small, then just the tumor can be removed, if it is in the correct location to remove it without damaging any other part of the eye. "If the tumor is large... and cause severe eye pain" the whole eye will be removed, medically referred to as enucleation ("Treating Uveal (Eye) Melanoma by Location and Size", 2017, para. 8). Once the removal of the eye occurs, after the patient heals, they would be fitted for a prosthetic eye that matches your other eye. The artificial eye can move, and resemble a real eye, but the patient will just lose their vision. Both radiation and surgery can result in sickness, much symptoms like the flu, and can sometimes lead to the loss of total vision. If the tumor metastasizes to the liver, there are treatments to try and reduce more metastasis and decrease the tumor, as well as after/before enucleation to try and stop metastasis. If the tumor is present, but has not metastasized, the oncologist can prescribe medication to prevent metastasis. "LS 2616, a quinoline 3–carboxamide... decrease in primary and secondary tumor's growth and metastasis" (Harning, 1988, p.1). It can slow the growth of the tumor that metastasized to the liver, the goal overall is to stop more metastases from ... Get more on HelpWriting.net ...
  • 14. Pharmacological And Ethnobotanical Review Of Aristolochia... Pharmacological and Ethnobotanical review of Aristolochia bracteolata L. (Aristolochiaceae) M. B. Patil Department of Botany, J.E.S's, Arts, Science and Commerce College, Nandurbar E–mail; drmadhukarpatil@gmail.com Abstract The present study deals with review of pharmacological and ethnobotanical uses of Aristolochia bracteolata L. from family Aristolochiaceae is commonly known as Kida–mari, Gidan–pala. The plant has been used widely by traditional practitioners for the treatment of various diseases in in Indian subcontinent in the traditional system of medicine to treat cholera, fever, bowel troubles, ulcers, leprosy, skin diseases, menstrual problems and snakebites. The plant is also used as emmenagogue, abortifacient, antineoplastic, antiseptic, anti–inflammatory, antimicrobial, antipyretic, antifertility and antispermatogenic agent. Aristolochic acid, a major active constituent of the plant is reported to cause cancer, nephropathy, sister chromatid exchange and is a potent abortifacient. Aristolochia species are also used in China, Philippines, Cuba, Nigeria, East and West Africa, Caribbean island, and sub tropical countries as a folk medicine to treat eczema, rheumatic pain, stomachic, earache, syphilis and gonorrhea. The plants also used in the treatment of domestic animals. The present review deals with the different scientific studies and reports available in different aspects of this plant in the areas of Morphology, Phytochemistry, Pharmacology, ... Get more on HelpWriting.net ...
  • 15. Trimethoxynicotinonitrile Essay 11– 4,5,6–Trimethoxynicotinonitrile–2–thion (39) was prepared through the multicomponent, condensation of acetaldehyde, cyanothio acetamide, 1–(butenyl)pyrrolidine. Compound (39) reacted with some alkyl halides yielding 2–alkylsulfanyl nicotinonitriles (40)106, scheme 41. 12– The one‐pot multicomponent condensation of malononitrile, 4‐methyl–pentan‐2‐one, aryl aldehyde, and ammonium acetate in ethanol yielded the 2‐amino‐5‐isopropyl‐4‐(4‐aryl)‐6‐methyl nicotinonitriles (41 a–f), which exhibited weak antioxidant activity107, scheme 42. 1.3.3. Catalysis mediated Synthesis of nicotinonitriles 1– The ammoxidation of 3–picoline to 3–nicotinonitrile (42) was induced by the influence of industrially synthesized and shaped vanadium phosphate... Show more content on Helpwriting.net ... L. Zhu et. al., reported the synthesis of new derivatives of 4–aryl–3,5–dicyano–2,6–di(3′–indolyl)pyridine (50) and polysubstituted (3′–indolyl)pyrazolo[3,4–b]pyridine and (3′–indolyl)benzo[h]quinolines (51) via a one–pot multicomponent reaction of aromatic aldehydes, 3–cyanoacetyl indoles, and ammonium acetate employing the microwave irradiation as an energy source and ethylene glycol as a solvent,115,116 scheme 50. 2– A series of 4–aryl–6–(indol–3–yl)–2,2–bipyridine–5–carbonitrile derivatives (52) were synthesized within shorter reaction time and high product yield via a one–pot multicomponent reaction of aromatic aldehydes, 3–(cyanoacetyl)indole, and 2–acetyl pyridine in ammonium acetate by microwave irradiation in solvent–free condition. The same conditions were applied for the synthesis of anther series of di(indol–3–yl)–diaryl bipyridine–dicarbonitrile derivatives (53a–e) using cinnamils, 3–cyanoacetyl indole and ammonium acetate117, scheme ... Get more on HelpWriting.net ...
  • 16. What Is Amlodipine Impurity? AmlodipineImpurity–D3–ethyl 5–methyl 2–((2–aminoethoxy)methyl)–4–(2–chlorophenyl)–6–methylpyridine–3,5–dicarboxylate AmlodipineImpurity–Ediethyl 2–((2–aminoethoxy)methyl)–4–(2–chlorophenyl)–1,4–dihydro–6–methylpyridine–3,5–dicarboxylate AmlodipineImpurity–Fdimethyl 2–((2–aminoethoxy)methyl)–4–(2–chlorophenyl)–1,4–dihydro–6–methylpyridine–3,5–dicarboxylate AmlodipineImpurity–I3–ethyl 5–methyl 2–((2–aminoethoxy)methyl)–4–(4–chlorophenyl)–1,4–dihydro–6–methylpyridine–3,5–dicarboxylate Aripiprazolen–oxide7–{4–[4–(2,3–dichlorophenyl)piperazin–1–yl]butoxy–n–oxide}–3,4–dihydroquinolin–2(1H)–one. AspartaneImpurity–A2–(5–benzyl–3,6–dioxopiperazin–2–yl)acetic acid. AtenololImpurity–A2–(4–hydroxyphenyl)acetamide AtenololImpurity–B2–(4–((oxiran–2–yl)methoxy)phenyl)acetamide ... Show more content on Helpwriting.net ... Memantine1–chloro–3,5–Dimethyl Adamantane1–chloro–3,5–dimethyladamantane Memantine1–Hydroxy–3,5–Dimethyl Admanatane3,5–dimethyladamantan–1–ol. MemantineImpurity–D1–Methyl Adamanatane MemantineImpurity–E1,3,5–Trimethyl adamentine MemantineN–Formyl memantine1–formyl memantine Memantine1–hydroxy 3,5–dimethyl adamantane1–hydroxy 3,5–dimethyl adamantane MetamizoleAcetyl metamizoleN–(2,5–dihydro–2,3–dimethyl–5–oxo–1–phenyl–1H–pyrazol–4–yl)acetamide MetamizoleImpurity–AN–(2,5–dihydro–2,3–dimethyl–5–oxo–1–phenyl–1H–pyrazol–4–yl)formamide MetamizoleImpurity–C ... Get more on HelpWriting.net ...
  • 17. Dual ACC1 / ACC2 Inhibition A general trend in dual ACC1/ACC2 inhibition was often encountered among the 125 compounds tested: good ACC1 inhibition was linked to good ACC2 inhibition.4 The same group elaborated on this study by examining the structure–activity relationship (SAR) for the pyrazole part and the substitution at position 9 of the 1,9–diazaspiro[5.5]– undecane. In this study, additional pharmacokinetics were studied along with the IC50 values for ACC1 and ACC2, such as the lipophilic ligand efficiency (LipE), measured lipophilicity (ElogD), human liver microsomal incubation (HLM), and passive permeability (Papp) in Ralph Russ canine kidney cells.6 1,9–Diazaspiro[5.5]undecan–2–one 1c (Fig. 4) was selected for a SAR study of the effects of ... Show more content on Helpwriting.net ... The downside was the poor Papp value obtained for compound 1h when compared to compound 1g. Compound 1i showed reasonable LipE values and diminished ACC inhibition (74 and 29 nM for ACC1 and ACC2, respectively), but a greatly increased Papp value of 9.7 (Г—10–6 cm/s) vs 0.8 for compound 1h. Based on these results, a further SAR study was performed by using isoquinolines and quinolines as Figure 4. Compounds used for studying the SAR for ACC inhibition with respect to the substitution at position 9 of the 1,9–diazaspiro– [5.5]undecane ring system. N H N c Me Me N
  • 18. H N d Cl N H N e CF3 H N f Cl H N g Cl N N H Cl N OMe N OMe N N NHMe
  • 19. h i j OMe N N NHPr NHMek l m n N NMe2 o N R O NHN t–BuN O N O NH N H N O N N i–Pr 1a o 2
  • 20. N H N N N H a b R = Chemistry of Heterocyclic Compounds 2017, 53(8), 827–845 830 substituents (compounds 1j–o). The development of amino– substituted species 1l–o did result in improved thermo– dynamic solubility at pH 1.2 with a factor up to 10 when compared to compounds 1j,k. The Papp values of com– pounds 1l,m were as bad as those of compound 1h. Efforts to improve Papp by increasing the alkylation on the amine led to compounds 1n,o exhibiting better Papp than com– pounds 1l,m. The Papp values of compounds 1n,o were still lower than those obtained for compounds 1j,k and, in addition, HLM clearance significantly worsened. Com– pounds 1j,k were chosen for in vivo examination of their ... Get more on HelpWriting.net ...
  • 21. Malaria Is A Parasite That Has Been Impacting The World... Malaria is a parasite that has been impacting the world for the past couple of centuries. The illness associated with malaria gives intense fevers, chills, terrible headaches, muscle pains and can be deadly if not treated properly. Although overall malaria cases have decreased from 262 million in 2000 to 214 million in 2015, it is still an issue to be concerned about today.1 There have been developments of a vaccine against this parasite, but the parasite has adapted to the vaccine and developed a resistance to it, thus rendering it ineffective. The p. falciparum and p. vivax strains of malaria is what is causing problems as these resistant strains have popped up in much of Asia and Africa and a couple of countries in South America.1 This can potentially be a problem for the military and more specifically the Air Force as multiple countries where the Air Force deploys are infected with these resistant strains of malaria. It can be seen through the background and history of the fight against this parasite that the chemistry behind an antimalarial vaccine is important to the Air Force. The illness associated with the malaria parasite was first thought to be a result of poisonous mists drifting from marshes hence its name meaning "bad air" in Italian. Of course it was unbeknownst back then that it was actually caused by the female anopheles mosquito which tends to live near still water such as marshes.2 Although it was unknown what actually caused the symptoms of malaria, ... Get more on HelpWriting.net ...
  • 22. The Role of Infections and Diseases in the Evolution of... Haldane's hypothesis which states that there is a role of infections or diseases as a driving force in the evolution of Metazoans is simply put as infection is a selective in the evolution of Metazoans and essential for the survival of certain populations. Malaria represents one of the most important selective factors affecting human populations. There are several inherited diseases of red blood cells that lead to resistance at the erythrocytic stage. О±–Spectrin Hereditary Elliptocytosis Hereditary elliptocytosis is a heterogeneous group of red–cell disorders characterized morphologically by oval–shaped erythrocytes (Gallagher, 2005). Ovalocytosis is an uncommon variant of hereditary elliptocytosis (Gallagher, 2005). It is caused by heterozygosity for a 27–base pair deletion in the gene encoding the erythrocyte membrane protein band 3 (SLC4A1∆27) (Williams, 2006) on chromosome 17 (Jarolim et al., 1991). A mutation results in impaired function and gross skeletal disruption of the membrane skeleton of the erythrocyte (Coetzer et al., 1990). It confers highly specific protection against cerebral malaria by maintaining similar parasitemia levels (Coetzer et al., 1990). The heterozygotic form is asymptotic (Coetzer et al., 1990). Ovalocytic erythrocytes are very rigid and relatively resistant to invasion by various strains of malarial parasites (Coetzer et al., 1990). There are four О±–spectrin mutations namely alpha 1/74, alpha 1/46, alpha 1/65 and alpha 1/61 (Coetzer et al., ... Get more on HelpWriting.net ...
  • 23. Research Paper On Pyrrolo 5.1. Introduction to Pyrrolo[1,2–a]quinoline The chemistry of fused nitrogen heterocycles is very important because of their occurrence in numerous natural products and their versatile applications in the pharmaceutical industry and materials science 1. Among various synthetic approaches for fused nitrogen heterocycles, pyrrolo[1,2–a]quinolines and their oxidized and reduced forms are widespread among natural products and biologically active pharmaceuticals 2. Moreover, the skeleton of pyrrolo[1,2–a]quinoline exists in many biologically active natural alkaloids such as gephyrotoxin (Fig. 5.1), which is a substituted perhydropyrrolo[1,2–a]quinoline that was isolated by Daly and co–workers in 1977 from secretions of the frog Dendrobates histrionics 3 Moreover, the isolation of gephyrotoxin a natural alkaloid with pyrrolo[1,2a]quinoline skeleton, which was subjected to numerous studies to investigate its biological activity and has been a target for total synthesis 4. Scheme 1. A few examples of pyrrolo[1,2–a]quinoline–containing natural products and pharmaceuticals. Pyrrolo[1,2–a]quinoline (Fig 5.2) and synthesis of its derivatives were reviewed in 2003 by El–Sayed and El–Sayed 5. In literature, new methods or the ... Show more content on Helpwriting.net ... An efficient method for the synthesis of fourteen novel diversified pyrrolo[1,2–a]quinoline derivatives has been described using 4–(1,3–dioxolan–2–yl)quinoline and different phenacyl bromides in acetone and followed by reacting with different acetylenes in DMF/K2CO3. The structure of the newly synthesized compounds was determined by IR, 1H NMR, 13C NMR, mass spectrometry and elemental analysis. The in vitro antioxidant activity revealed that, among all the tested compounds 5n has exhibited maximum scavenging activity with ABTS. The compound 5b has showed good antiproliferative activity as good inhibitor of EGFR tyrosine ... Get more on HelpWriting.net ...
  • 24. Tattoos Research Tattoos have a history that extends far back into the furthest reaches of time. For millennia tattoos have been used to help differentiate members of tribes and regions and even of religions. But the concept of tattooing did not catch on in the Western world until 18th century explorers discovered "tatau" in Polynesia; a technique that became popular among European sailors and then spread to the general populace of Western societies. Tattoos are made by inserting indelible ink into the skin's dermis layer in order to change the skin's pigmentation for (usually) decorative reasons. In some places and times tattoos were created by hand–tapping the ink into the skin. This could be done with sharpened sticks, bones or any sufficiently sharp object. More modern times have ... Show more content on Helpwriting.net ... The tattoo artist uses a stencil to draw the design onto the skin, and then outlines it with a single–tipped needle and thin ink. Shading is then done using a thicker ink and a variety of needles and color can be applied, this is usually done more than once to ensure even coloring. With the advent of computers to produce high quality tattoo flashes, the improvements in tattoo designs have been quite impressive, ranging from complex single–line designs to impressively blended black and gray shading, sharply delineated colors and realistic portraiture, all of which are a far cry from the blue and black fuzzily outlined tattoos of years gone by. And while anyone can learn to use tattoo equipment, it still takes a real artist to create true tattoo art and the true portfolio of a real artist is not in how many tattoo flashes they have on their walls, nor even in the equipment they have on hand, but on the number of satisfied customers they have ... Get more on HelpWriting.net ...
  • 25. The Effects Of Malaria On African Continent And Is... Malaria is a life–threatening disease that is caused by plasmodium parasites transmitted from female mosquitos when they bite a human. The plasmodium parasite can also be transmitted by blood products like unclean needles or unscreened blood. There are five parasite species (Plasmodium, falciparum, P. vivax, P. ovale, and P. malariae) that causemalaria in humans, and two of these species, P. falciparum and P. vivax, are the greatest threat (see Figure 1). The severity of malaria is based on the species of plasmodium. The symptoms people experience include chills, fever, and sweating usually occurring within a few weeks after being bitten. In the United States, it is a very rare disease with fewer than 20,000 cases per year, and is treatable by a medical professional. However, Sub–Saharan Africa is home to 88% of malaria cases and 90% of malaria deaths. P. falciparum is the most prevalent parasite on the African continent and is responsible for most malaria–related deaths globally. P. vivax is more widely distributed than P. falciparum and predominates in most countries outside of Africa. In the 1970s and 1980s, resistance of P. falciparum started in medicines, such as chloroquine and sulfadoxine–pyrimethamine (SP). Drug resistance has been implicated in the spread of malaria to new areas and re–emergence of malaria in areas where the disease had been eradicated. Population movement has introduced resistant parasites to areas previously free of drug resistance. Resistance is ... Get more on HelpWriting.net ...
  • 26. Nucleophilic Reaction Lab Report March 2017 Selective Synthesis Dispiro[indoline–3,2′–pyrrolidine–3′,3″–quinoline] Derivatives and Spiro[imidazole–4,3′–quinoline] Derivatives via 1,3–Dipolar Cycloaddition Reaction 859 M niv am cem 02/ On e–3 de cycloadditio structure 4 The target compound 7 was prepared by adding the re– ortion. The poxide for– ave methyl © 2016 Wiley Periodicals, Inc. nitrogen atom from sarcosine and carbonyl of isatin, 4–hydroxy–7–methoxy–2–oxo–1,2–dihydroquinoline–3–carbo for this reaction, leading to the formed spiro . The nucleophilic reaction between the Moreover, the treatment of compound 9 w disulphide in the presence of dimethylsulphate g Chemistry. The 1,3–dipolar cycloaddition reaction of azomethine ylide b with dipolarophile 3 yielded ... Show more content on Helpwriting.net ... Anal. for C28H25N3O5 (483.18): Calcd: C
  • 27. 69.55, H 5.21, N 8.69%. Found: C 69.59, H 5.19, N 8.50%. 2–Amino–7′–methoxy–5–(4–methoxyphenyl)–2′H–spiro[imidazole– 4,3′–quinoline]–2′,4′ (1′H)–dione (7). A mixture of 3 (1.0 g, 3.23mmol), H2O2 (0.37mL, 30%), and ethanol (20mL) was stirred at room temperature then added guanidine nitrate (0.59 g, 4.83mmol) and aqueous solution of KOH (50%) (1.30mL) were stirred at 80В°C for 2 h. The ethanol was evaporated, and water (30mL) was added to the reaction mixture remainder. The outcome product was п¬Ѓltered off, washed accurately with water. The wet product slightly still wet п¬Ѓlter cover was mixed with ethanol (10mL), and the resulted suspension refluxed for 30min. After cooling, the precipitate was п¬Ѓltered off, washed with ethanol, and п¬Ѓnally dried. Yellow crystals (0.35 g, 30%), mp 196–197В°C (DMF/ H2O); Rf = 0.63 [ethyl acetate: pet. ether (40:60)](1.5:4); IR(KBr): Оі/cmпїЅ1 = 3327 (NH2), 3267 (NH), 1658 (CO), 1612 (CONH); 1H NMR (CDCl3): Оґ: 3.72 (s, 3H, OCH3– quinolone), 3.83 (s, 3H, OCH3–aromatic), 6.77–6.89 (m, 7H, aromatic–CH), 7.87 (broad s, 1H, NH, D2O exchange– able), 9.83 (broad s, 2H, NH2, D2O exchangeable); ... Get more on HelpWriting.net ...
  • 28. The Most First Time Of Zopf The very first time, Zopf was described the genus Rhodococcus in 1981 and then redefined in 1977 to accommodate a number of strains that resembled but did not belong to the genera Corynebacterium, Mycobacterium and Nocardia.1, 2 Thereafter, considerable changes were made to the classification of the genus. Some species have been combined, some reclassified in new genera and new species have also been described.1 at present there are over 40 species classified under the genus Rhodococcus.3–4 The genus Rhodococcus are aerobic, GC– rich nonsporulating, non motile Gram–Positive bacteria which also contain mycolic acids in their cell envelope.5–7 The cell wall of rhodococci are chemotype IV, means the peptidoglycan is mesodiaminopimelic acid... Show more content on Helpwriting.net ... For instance, the production of acrylamide from acrylonitrile by using Rhodococcus rhodochrous J1.13 Rhodococci present a unique enzymatic capabilities, for instance Rhodococcus erythropolis produce large number of enzymes that allow them to undergo the reactions like bioconversation and biodegradations.14 Biosurfactants and bioflocculants Rhodococci have the ability to produce surfactant molecules, which contain strong hydrophilic and hydrophobic groups and also migrate to interfaces between oil and aqueous phases. Some biosurfactants, including some Rhodococcus produced surfactants that are more efficient, more degradable and less toxic than synthetic surfactants. The relevance of surfactants to biodegradation of pollutants is threefold; the cellular surfactants cause adherence of rhodococci to hydrophobic phases in two phases and surfactants lower the interfacial tension between the phases, making it easier for hydrophobic compounds to enter the cell. At the same time extracellular surfactants disperse hydrophobic compounds that increase the surface area for the attachment of mycolic acids.1 ... Get more on HelpWriting.net ...
  • 29. INTRODUCTION:- HISTORICAL BACKGROUND OF ANTIHYPERTENSIVE... INTRODUCTION:– HISTORICAL BACKGROUND OF ANTIHYPERTENSIVE THERAPY Antihypertensive therapy with the conventional drugs such as thiazide diuretics,beta –adrenoreceptor antagonists and Calcium channel antagonist (CCA ) based regimens can reduce the risk of stroke and other cardiovascular events. The drugs used as first line therapy in both younger and elderly patients include the conventional drugs such as diuretics, CCA or ACE inhibitors based regimens[6][7] ACE inhibitors such as Captopril and enalapril are used clinically for the treatment of hypertension and congestive heart failure(CHF). Despite the fact that ACE inhibitors have met with a high degree of success, ACE is a nonspecific protease responsible for degradation of bradykinin... Show more content on Helpwriting.net ... So we got an idea to synthesize some new AT1 receptor antagonists which do not have these side effects. RENIN ANGIOTENSIN ALDOSTERONE SYSTEM:– [13] The renin angiotensin system is one of the powerful regulators of blood pressure and volume homeostatis. Renin is a proleolytic enzyme which is produced in the juxtaglomerular apparatus of the kidney. It acts on the angiotensinogen which is a–globulin produced by the liver. Then there is a formation of Angiotensin 1 (decapeptide) Asp–Arg–Val–Tyr–Ile–His–Pro–Phe–His–Leu. Ang1 has little biological activity. Then Angiotensin is produced when there is removal of the C –terminal dipeptide Histidyleucine from Ang 1 by the action of metalloprotease enzyme ACE (Angiotensin converting enzyme) mainly present in lungs and Angiotensin II (1–8) is produced which is an octapeptide in regulating the mineralocorticoids, it induces the sodium and water retention in the body. ANGIOTENSIN II RECEPTOR BLOCKERS:– Angiotensin II receptor blockers (ARBs) (eg, valsartan, losartan, candesartan, telmisartan, tolmesartan, and irbesartan) act by selectively blocking the AT1 receptor, thereby directly blocking the vasoconstrictor and growth effects of Ang II.[16] Selective blockade of the AT1 receptor has additional cardiovascular benefits resulting in vasodilation, growth ... Get more on HelpWriting.net ...
  • 30. Air Pollution Is An Unavoidable Mixture Of Substances That... Air pollution is an unavoidable mixture of substances that we breathe in. There is no way to escape air pollution nowadays since it can be encountered indoors as well as outdoors. The type of pollution we breathe in can be divided between indoor and outdoor by the different types of air pollution that are released in these environments. Fine particles such as burning fossil fuels (such that come from traffic and energy production), tobacco smoke, and chemical vapors are found in the air breathed in from outdoors, while solvents (such as found in household cleaners and products), mold, and carbon monoxide are sadly breathed in from within homes and businesses on a daily basis. There is no question to anyone's mind that these air pollutants cause harmful effects to one's health. Studies have been conducted to link air pollution to the hundreds of ailments that many men, women and children have suffered over the years. Cardiovascular and respiratory illnesses are without a doubt caused by air pollution as studies have shown. Today there are studies showing thatAutism is linked to air pollution. The purpose of this paper is a review of the current state of knowledge on air pollution and whether it plays a role in children developing autism. Autism is a disability that impairs the normal brain development in children. It causes deficits in their verbal and non–verbal communication, social interaction, and play. Girls are more likely to show severe characteristics of the ... Get more on HelpWriting.net ...
  • 31. Synthesis Of Pi3k Inhibitors To start with, the synthesis of class I and class III phosphoinositide 3–kinase inhibitors has become a much–needed research process. Creating and modifying the PI3K inhibitors through the addition and elimination of organic functional groups or amino acids has allowed scientists to find the best way in attacking the irregularities formed in the body. Plenty of class I PI3K inhibitors– like those seen in Figure 3– have been identified and modified for therapeutic means. For example, GDC–0941 and BKM–120 are both inhibitors that are being considered as possible clinical trial candidates [2]. Other inhibitors have also been developed for specific PI3K isoforms which helps to highlight the usefulness of the PI3K pathways [2]. To get a better... Show more content on Helpwriting.net ... In the studies being done, scientists realized that the BKM–120 inhibitor not only affects the PI3K/PKB/mTOR pathway, but the microtubule synthesis pathway, as well [5]. This dual activity found in the BMK–120 inhibitor was due to the structure of the inhibitor; Figure 5 illustrates how these two functions are possible (a) and what the ratio of microtubule inhibition and PI3K inhibition are in the cell (b) [5]. Through extensive studies on the BMK–120 inhibitor and other similar compound structures, researchers, like Bohancker et al., have been able to identify key structural components for the two activities. The Bohancker et al. found that additional nitrogen in the core of the molecule could help remove the tubulin inhibition, as well as, less symmetry in the BMK–120 overall structure [5]. In general, the research being done in these two examples, and the many other inhibitor synthesis experiments, show how the creation and modification of the phosphoinositide 3–kinases inhibitors is a huge part PI3K studies. From these developments, scientists can get a better sense of how the inhibitors will work in cells and treating diseases. Though the synthesis of phosphoinositide 3–kinase inhibitors is necessary for advancements in this field, research on how efficient and effective these inhibitors are is just as imperative. Many assays have been developed to study the effectiveness of PI3Ks– mainly through the quantifying of kinase ... Get more on HelpWriting.net ...
  • 32. Biodegradation of Hydrocarbons from Crude Oil by... Biodegradation of Hydrocarbons from Crude Oil by Pseudomonas putida A Project done under the guidance of Dr. K. Bharathi Department of Biotechnology. Submitted to the faculty Of Department of Biotechnology National Institute Of Technology, Warangal (A.P) Submitted By Febin P. Nalpady, Anzal Rahman, Shruti Sharma, Sindhuja Nandiraju, Giraboina Kranthi Kumar NATIONAL INSTITUTE OF TECHNOLOGY WARANGAL (A.P) (DEEMED UNIVERSITY) 2010–2011 ... Show more content on Helpwriting.net ... 2.Introduction In quantitative terms, crude oil is one of the most important organic pollutants in marine environment and it has been estimated that worldwide somewhere between 1.7– 8.8Г—106 tons of petroleum hydrocarbons impact marine waters and estuaries annually. Reports have been appearing since last three decades on the biodegradability of crude oil by bacteria which can use hydrocarbons as source of carbon and energy. A way to mitigate the effects of oil spills is bioremediation. 2.1 Bioremediation It is a process by which chemical substances are degraded by bacteria and other microorganisms. The use of these microorganisms has been successfully applied for the treatment of waste and wastewater in controlled systems. Several research studies have recently been performed to investigate the use of bioremediation for oil–spill cleanup in seawater, freshwater and terrestrial areas. The technique has been found to have a potential for broad applications in terrestrial and freshwater environments for treating soils and sediments contaminated with oil and other substances, as well as for coastal environments impacted by oil spills. Water is a more sensitive medium than soil and requires different remediation techniques. Spills to surface water are easier to clean up than spills to groundwater, for obvious reasons. It is not only much harder to see the extent of the contamination, but also to remove the source of the contamination as, for ... Get more on HelpWriting.net ...
  • 33. Advantages And Disadvantages Of Benzofuran INTRODUCTION: The metal chelates of various ligands play pivotal role in many important medicinal applications. They also useful for metal extraction and detection. The present aspect is context to the novel heterocyclic ligand containing .pharmaceutica active segments like benzofuran, 1,3,4–oxadiazoe and p–amino salicylic acid as ligand. So the literbture review is as follow: LITERATURE REVIEW:Chelating agents, because of their metal specificity or selectivity, can function as good flotaids and selective flocculants. In addition to the metal selectivity, chelating agents offer certain advantages over conventional mineral processing reagents even from the synthesis point of view. With the major donor .atoms–S, N, 0 and, to some extent, P–numerous possibilities exist to tailor make reagents for specific applications.[1–3] For polymers the backbone offers further possibilities for the incorporation of the required properties. In general, the choice of a chelating agent or a group is made on the basis of its function in well–known analytical metal separations. Such a choice is limited in that the number of well–known ... Show more content on Helpwriting.net ... Objectives: a.The objectives of the proposed work are To synthesis : and characterize benzofuran–1–;3,4–oxadiazole–p–amno salicylic acid ligands. b.To prepare the metal, chelates of above ligands and stheir characterization WORK PLAN: Following work will be carry out Synthesis of Benzofuran–1,3,4–oxadiazole derivative The Mannich reaction of above derivative with p–aminosalicylic acid Characterization of all the derivatives. The transition metal chelates preparation and characterization by metal:ligand ratio, spectral study and magnetic properties. Testing of microbicidal ... Get more on HelpWriting.net ...
  • 34. Different Definitions Of Key Terms Definitions of key terms However, looking at the conceptual perspective, Colwell, R. R., and J. D. Walker (1977, cited in Aniefiok E. Ite1, et al., 2013: p 78 –79) defines oil as follows: "Oil is a naturally stirring multipart mixture made up primarily of hydrocarbon mixtures and normally contains substantial quantities of nitrogen, sulphur, and oxygen together with smaller amounts of nickel, vanadium, and numerous components. Oil compounds can occur in solid form as asphalt, liquid form as crude oil and/or gaseous form as natural gas. Petroleum hydrocarbons could be divided into four classes: saturates (pentane, hexadecane, octacosane, cyclohexane), aromatics (naphthalene, phenanthrene, benzene, pyrene), asphaltenes (phenols, fatty acids, ketones, esters, and porphyrins), and resins (pyridines, quinolines, carbazoles, sulfoxides and amides)". : P 78–79 Natural gas is the world 's third major energy source, estimated at 21% of total prime energy usage (www.indexmundi.com/commodities/market). On the other hand, environmental risks are consequences that result from oil exploration to the communities (e.g. workers, consumers and local people). CHAPTER TWO LITERATURE REVIEW 2.0 Introduction This chapter focuses on what other scholars have written about risks associated with oil and gas exploration, drilling and extraction in various parts of the World. The chapter is structured in accordance with the objectives of the study, that is, to assess the ... Get more on HelpWriting.net ...
  • 35. Symptoms And Treatment Of Alzheimer 's Disease Introduction The neurodegenerative disorder Alzheimer's Disease (AD) is currently the most common cause of dementia and affects millions of people around the world.В№ There are multiple risk factors associated with AD, including genetic factors, hypertension, diet and most significantly, age. Individuals over the age of 65 are most vulnerable to the disease and at this point, the risk increases every 5 years.В№ Alzheimer's Disease was first described over 100 years ago by Alois Alzheimer in Germany, characterising the first case with memory impairments and the presence of neuropathological plaques and tangles, which today, are major indications of the disease.ВІ Progressive memory loss is the clinical trademark of AD but eventually, cognitive function also deteriorates.Ві The neuropathological trademarks of AD involve the accumulation of ОІ amyloid (AОІ) proteins expressed as plaques and the phosphorylation of tau proteins expressed as neurofibrillary tangles.Ві The formation of these plaques and tangles are estimated to begin 20 years before clinical symptoms arise.ВІ MRI studies have shown the association of AD with hippocampal atrophy, however, it remains difficult to distinguish from other forms of dementia.вЃґ However, this pathology is also known to be present without the impairment of cognitive function.вЃµ Recently, there has been a number of studies investigating this incongruity between pathology and cognition, all of which reported similar dissonance, remarkably in older ... Get more on HelpWriting.net ...